The Ligandable Human Proteome

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Bromodomain-containing protein 4

Bromodomain

IndexLigand NameStructurePDB codeligand desolvation
1etuBivalent binding to BET bromodomains5ad292.22
2cpbCrystal structure of the first bromodomain of human BRD4 in complex with FLAVOPIRIDOL4o7188.16
38ngBRD4_Bromodomain1-A13768555uvw87.95
4b0qCrystal structure of human BRD4(1) bromodomain in complex with UT22B5oww85.03
51m3Crystal structure of the first bromodomain of human BRD4 in complex with TG1012094o7684.96
687pBRD4_BD2_A-13599305uer82.33
72taCrystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor TG-1013484ogj82.1
887mBRD4_BD2_A-13901465ueq81.98
987gBRD4_BD2_A-13950175ueo81.18
100s6Crystal structure of the second bromodomain of human BRD4 in complex with MS417 inhibitor6duv80.73
111h3Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand4j0s79.18
121h2Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand4j0r78.84
1389dBRD4_BD2_A-14976275uex78.47
141qkCrystal structure of the first bromodomain of human BRD4 in complex with DINACICLIB4o7078.29
15rnkN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 4-chloro-2-methyl-5-(((3-methylthiophen-2-yl)methyl)amino)pyridazin-3(2H)-one5mkz78.29
169e3Crystal Structure of the first bromodomain of human BRD4 in complex with 5-((4-fluoro-1H-imidazol-1-yl)methyl)quinolin-8-ol6afr78.29
175ouFIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR 3-(4-Chlorobenzyl)-7-ethyl-3,7-dihydropurine-2,6-dione5eis78.21
18dyzFIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR F16fnx78.19
1925kCrystal Structure of the first bromodomain of human BRD4 in complex with a 5-methyl-triazolopyrimidine ligand4men78.15
2088mBRD4_BD2_A-14128385uey77.88
2114zCrystal Structure of the first bromodomain of human BRD4 in complex with a quinazoline ligand4hbw77.81
22e5tCrystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand6ft377.76
23l26First bromodomain of BRD4 bound to inhibitor XD265d2477.64
24e5qCrystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand6fsy77.45
255nvFirst 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-dione5ei477.34
268nvBRD4_BD2_A-14540565uvt77.26
2730mCrystal structure of the first bromodomain of human BRD4 in complex with Olinone4qb377.21
288nsBRD4 Bromodomain 2 with A-14570665uvv77.1
2979cCRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH RO32805vbp77.06
308o4BRD4_BD2_A-14610285uvu76.81
3177xStructure of the first bromodomain of BRD4 with a pyrazolo[4,3-c]pyridin fragment5luu76.71
32hccCrystal structure of BRD4 in complex with isoliquiritigenin and DMSO (Cocktail No. 3)6ajv76.66
3364sCrystal structure of fragment bound with Brd45hq776.35
34p9lN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 1,3-DIMETHYL-6-(MORPHOLINE- 4-SULFONYL)-1,2,3,4-TETRAHYDROQUINAZOLIN-2-ONE4a9l75.8
3589jBRD4_BD2-A-351655uf075.75
363x0Discovery of benzotriazolo diazepines as orally-active inhibitors of BET bromodomains: Crystal structure of BRD4 with CPI-134x2i75.67
3756yFirst bromodomain of BRD4 bound to inhibitor XD475d3t75.53
38foyBRD4(BD1) complexed with 27596czv75.41
3914xCrystal Structure of the first bromodomain of human BRD4 in complex with a quinazolin ligand4hbx75.34
4062vCrystal structure of the first bromodomain of human BRD4 bound to benzoisoxazoloazepine 35hm075.24
4169gBRD4 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)5i8875.22
422n0Crystal Structure of the first bromodomain of human BRD4 in complex with compound B134pce75.19
432rfCrystal structure of the first bromodomain of human BRD4 in complex with SB-4095144o7a74.99
4408hCrystal Structure of the first bromodomain of human BRD4 in complex with Alprazolam3u5j74.8
45gujBRD4 bromodomain 1 in complex with HYB1576dl274.78
46d7tHuman BRD4 C-terminal bromodomain with 1-(4-(3-methylbenzyl)-3,4-dihydroquinoxalin-1(2H)-yl)ethanone6ffd74.76
4708kCrystal Structure of the first bromodomain of human BRD4 in complex with a benzo-triazepine ligand (BzT-7)3u5l74.59
482rjCrystal structure of the first bromodomain of human BRD4 in complex with SB-284847-BT4o7b74.21
49e0kCrystal Structure Analysis of the BRD45yqx74.08
507uuComplex structure of the first bromodomain of BRD4 with an inhibitor that containing a 2H-chromen-2-one ring5wuu73.85
51fp7BRD4(BD1) complexed with 32196czu73.5
5289gBRD4_BD2_A-13428435uez73.45
53h4cDiscovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains4c6673.32
54rmrTrimethoxy-ring inhibitor in complex with the first bromodomain of BRD45h2173.17
55a0rCrystal structure of BRD4 in complex with 2',4'-dihydroxy-2-methoxychalcone6ajy73.08
56e5wCrystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand6ft472.84
572sjCrystal Structure of BRD4(1) bound to Colchiceine4lys72.8
588f6BRD4 bound with compound Bdi35xi372.71
595w4Crystal structure of the first bromodomain of human BRD4 in complex with PNZ5 isoxazole inhibitor5fbx72.38
60bmfCrystal structure of the first bromodomain of human BRD4 in complex with bromosporine (BSP)5igk72.05
610q1Crystal Structure of the first bromodomain of human BRD4 in complex with a isoxazolylbenzimidazole ligand4gpj72.04
626jfN-terminal bromodomain of BRD4 in complex with OTX-0155wmg71.6
637e7Crystal structure of BRD4 BROMODOMAIN 1 IN COMPLEX WITH LIGAND 25m3a71.48
6408jCrystal Structure of the first bromodomain of human BRD4 in complex with Midazolam3u5k71.48
658njBRD4 Bromodomain 2 with A-13493915uvy71.46
66y81Crystal structure of human BRD4(1) in complex with 4-[(5-phenylpyridin-3-yl)carbonyl]-3,4-dihydroquinoxalin-2(1H)-one (compound 19d)4yh471.42
675v2N-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-carboximidamide4uiy71.39
6813fCrystal Structure of the first bromodomain of human BRD4 in complex with a quinazolin ligand4hby71.19
69savCrystal structure of the first bromodomain of human BRD4 in complex with GW612286X4o7871.13
70tvuN-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- carboxamide4uix71.06
7196xThe first bromodomain of BRD4 with compound BDF-12535z5v71.04
7262gCrystal structure of the first bromodomain of human BRD4 bound to CPI-06105hls70.95
73r78Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor BI-25364ogi70.76
742rqCrystal structure of the first bromodomain of human BRD4 in complex with SB-2515274o7f70.6
7557eFirst bromodomain of BRD4 bound to inhibitor XD415d3p70.56
768f9BRD4 bound with compound Bdi25xi270.56
77e0bCrystal Structure of the first bromodomain of human BRD4 in complex with benzo[cd]indol-2(1H)-one ligand5d0c70.52
785w0Crystal structure of the first bromodomain of human BRD4 in complex with MA4-022-15f6170.48
7987sBRD4_BD2_A-13447725ues70.39
808f0BRD4 bound with compound Bdi45xi470.34
816rxCRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH A DIHYDROPYRIDOPYRIMIDINE SCAFFOLD INHIBITOR5kdh70.32
82jqyCrystal structure of the first bromodomain of human BRD4 in complex with SKT-68, a 1,4,5-trisubstituted imidazole analogue6mh770.27
838xxCrystal structure of BRD4-BD1 bound with hjp645you70.27
84jqpCRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH HU-10, A 1,4,5-Trisubstituted Imidazole Analogue6mh170.25
855vyCrystal structure of the first bromodomain of human BRD4 in complex with MA2-0145f5z70.18
868xrCrystal structure of BRD4-BD1 bound with hjp1265yov70.14
87wdrCrystal Structure of the first bromodomain of human BRD4 in complex with a dihydro-quinazolin ligand3svf69.57
88l40First bromodomain of BRD4 bound to inhibitor XD405d3n69.53
89hccCrystal structure of BRD4 in complex with isoliquiritigenin in the absence of DMSO6ajx69.42
904v1Crystal structure of hBRD4 in complex with BL-BI06 reveals a novel synthesized inhibitor that induces Beclin1-independent/ATG5-dependent autophagic cell death in breast cancer4zw169.22
911ghCrystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A)3zyu69.2
921xbStructure of BRD4 bromodomain 1 with a dimethyl thiophene isoxazole azepine carboxamide4lrg68.9
93579First bromodomain of BRD4 bound to inhibitor XD445d3s68.86
94eamCrystal Structure of the First Bromodomain of Human Brd4 in complex with IBET inhibitor3p5o68.55
954ldBRD4 bromodomain 2 in complex with gamma-carboline-containing compound, number 18.4z9368.46
9678jN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 8-(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-ylamino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one5a8567.8
97wshCrystal Structure of the First Bromodomain of Human Brd4 with the inhibitor GW841819X2yel67.43
9856mFirst bromodomain of BRD4 bound to inhibitor XD275d2567.37
99wshCrystal Structure of the Second Bromodomain of Human Brd4 with the inhibitor GW841819X2yem67.3
1000s6Crystal structure of the first bromodomain of human BRD4 in complex with MS417 inhibitor4f3i67.09
1018j2Crystal structure of the first bromodomain of human BRD4 in complex with a tetrahydroquinoline analogue5n2m67.04
102eo4BRD4 BD1 in complex with compound CF536c7r66.76
103bnjBrd4 Bromodomain 1 complex with its novel inhibitors4qr366.64
104jq1Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor JQ13mxf66.54
105y80Crystal 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)4yh366.44
1060s6BRD4_BD2_A-11076045ueu66.38
107np8NN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-5-methoxypyridin-3-yl-3- methyl-8-piperidin-4-ylamino-1,2-dihydro-1,7-naphthyridin-2-one5a5s66.19
1089gyBenzopiperazine BET bromodomain inhibitor in complex with BD1 of Brd45vom65.48
109eo1BRD4 BD2 in complex with compound CE2776c7q65.23
110bnmBrd4 Bromodomain 1 complex with its novel inhibitors4qr564.66
11157gFirst bromodomain of BRD4 bound to inhibitor XD295d3h64.52
1129bmThe first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand4bw364.05
1135d2FIRST 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-carboxamide5dlx63.95
114l33First bromodomain of BRD4 bound to inhibitor XD335d3j63.76
115bnkBrd4 Bromodomain 1 complex with its novel inhibitors4qr463.74
116locCrystal structure of the first bromodomain of BRD4 in complex with 18-Crown-66in163.15
1173p2Crystal 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)4wiv63.1
11873bN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH GSK1324726A (I-BET726)4bjx63.08
119locCrystal Structure of BRD4(1) bound to Colchicine4lzr63.01
1209bmA multiconformer ligand model of 3,5 dimethylisoxaxole bound to the bromodomain of human BRD46dml62.83
12157cFirst bromodomain of BRD4 bound to inhibitor XD425d3r62.75
12221qCrystal Structure of BRD4(1) bound to inhibitor XD144lyw62.7
12353wA multiconformer ligand model of inhibitor 53W bound to CREB binding protein bromodomain6dmj62.7
124locJoint nentron and X-ray structure of BRD4 in complex with colchicin6ajz62.67
125l28First bromodomain of BRD4 bound to inhibitor XD285d2662.58
126uthThe first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand4bw262.36
1275nqFIRST 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-dione5egu62.31
128s5bThe first bromodomain of human BRD4 in complex with 3,5 dimethylisoxaxole ligand4bw162.3
129837BRD4 first bromodomain (BD1) in complex with dual PI3 kinase (PI3K) inhibitor SF25355u2e62.11
13053wSelective pharmacological inhibition of the CREB binding protein bromodomain regulates inflammatory cytokines in macrophages and RGS4 in neurons5cfw62.11
131nueCrystal structure of the first bromodomain of human BRD4 in complex with MS267 inhibitor4nue61.9
1321k0Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-OH)4mr361.79
133dzhFIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR #176fo561.75
1343otDirect photocapture of bromodomains using tropolone chemical probes4whw61.51
13582yBRD4 first bromodomain (BD1) in complex with dual PI3 kinase (PI3K) inhibitor SF2558HA5u2f61.45
1362reCrystal structure of the first bromodomain of human BRD4 in complex with SB 2021904o7761.42
1371k0X-ray crystal structure of bromodomain complex to 1.24 A resolution4j3i61.36
138iesN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH I-BET2954cl960.54
139fzeN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH : 8-(((1R,2R,3R,5S)-2-(2-(4,4-difluorocyclohexyl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one6hdq60.32
140x27Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor JWG0566cj260.19
14183tN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH IBET-2954clb59.79
1426xxN-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)-one5lj159.71
1435w1Crystal structure of the first bromodomain of human BRD4 in complex with MA4-022-25f6259.56
144hg8Crystal structure of the first bromodomain of human BRD4 in complex with the inhibitor 16k6q3z59.53
1452rkCrystal structure of the first bromodomain of human BRD4 in complex with SB-614067-R4o7c59.2
1461k0Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-208)4mr459.19
1479s3N-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-one5acy59.13
1481a9Brd4 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 inhibitor4hxl59.02
1495vzCrystal structure of the first bromodomain of human BRD4 in complex with SG3-0145f6058.95
150n1dN-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-one4uiz58.89
1512llCrystal structure of the first bromodomain of human BRD4 in complex with an isoxazolyl-benzimidazole ligand4nr858.78
15257fFirst bromodomain of BRD4 bound to inhibitor XD355d3l58.52
1536jeN-terminal bromodomain of BRD4 in complex with OTX-0155wmd58.19
154ay2Crystal structure of human BRD4(1) bromodomain in complex with DR465ovb58.17
1556xhBRD4 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)5ku358.11
1568q9Crystal Structure Analysis of the BRD45y9357.45
1572taCrystal structure of the first bromodomain of human BRD4 in complex with TG1013484ps556.6
1585mjCrystal Structure of the First Bromodomain of Human BRD4 in Complex With Cyclic Vinylogous Amide Inhibitor MS4025ula56.2
159hg5Crystal structure of the first bromodomain of human BRD4 in complex with the inhibitor 16i6q3y56.01
160kszCrystal Structure of the first bromodomain of BRD4 in complex with a benzodiazepine ligand6s2555.44
1616tbCRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH DB-1-264-25kj054.68
162jbsCrystal structure of human BRD4(1) in complex with CN210 (compound 19)6mau54.67
1636xwN-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)-one5lj253.64
1644k4CRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH LRRK2-IN-15vbo53.53
165hryCrystal structure of human BRD4(1) in complex with CN7506e4a52.67
1664wgBRD4 in complex with ERK5 inhibitor XMD8-925lrq52.42
1675d1FIRST 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)butanamide5dlz52
1685gdX-ray crystal structure of human BRD4(BD1) in complex with RVX297 to 1.12 A resolution5dw251.78
1699u4BRD4-BD1 in complex with Cpd19 (3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide)5vzs49.58
170ex1Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor JWG0466cd448.44
1712loCrystal structure of BRD4 first bromodomain in complex with SGC-CBP30 chemical probe5bt448.4
172x30Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor JWG0485w5548.2
1734k4Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor XMD11-505wa547.47
174r78Crystal structure of the first bromodomain of human BRD4 in complex with BI 25364o7445.7