4KV4
 
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5UVW
 | | BRD4_Bromodomain1-A1376855 | | 分子名称: | Bromodomain-containing protein 4, N-[4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide, SULFATE ION | | 著者 | Park, C.H. | | 登録日 | 2017-02-20 | | 公開日 | 2017-06-21 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.14 Å) | | 主引用文献 | BRD4_Bromodomain1-A1376855
To Be Published
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4KV1
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5WMD
 | | N-terminal bromodomain of BRD4 in complex with OTX-015 | | 分子名称: | 2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide, Bromodomain-containing protein 4 | | 著者 | Zhang, Y. | | 登録日 | 2017-07-28 | | 公開日 | 2018-08-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.27 Å) | | 主引用文献 | BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.
Cancer Discov, 8, 2018
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5WMA
 | | N-terminal bromodomain of BRD4 in complex with PLX5981 | | 分子名称: | 1,2-ETHANEDIOL, 5-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-pyrrolo[2,3-b]pyridine, Bromodomain-containing protein 4 | | 著者 | Zhang, Y. | | 登録日 | 2017-07-28 | | 公開日 | 2018-08-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.401 Å) | | 主引用文献 | BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.
Cancer Discov, 8, 2018
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5WMG
 | | N-terminal bromodomain of BRD4 in complex with OTX-015 | | 分子名称: | 1,2-ETHANEDIOL, 4-{6-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1S)-1-(pyridin-2-yl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl}benzoic acid, Bromodomain-containing protein 4 | | 著者 | Zhang, Y. | | 登録日 | 2017-07-28 | | 公開日 | 2018-08-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.19 Å) | | 主引用文献 | BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.
Cancer Discov, 8, 2018
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6MNL
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6JJ6
 | | BRD4 in complex with 500 | | 分子名称: | 1-methyl-6-(3-(4-methylpiperazine-1-carbonyl)benzyl)-1,2a1,5a,6-tetrahydro-2H-pyrido[3',2':6,7]azepino[4,3,2-cd]isoindol-2-one, Bromodomain-containing protein 4 | | 著者 | Xu, J, Chen, Y, Jiang, F, Zhu, J. | | 登録日 | 2019-02-25 | | 公開日 | 2020-02-26 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | BRD4 in complex with ZZM1
To Be Published
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6JI3
 | | BRD4-BD1 bound with ligand 103 | | 分子名称: | (3~{R})-4-cyclopropyl-1,3-dimethyl-6-(1~{H}-pyrrol-2-yl)-3~{H}-quinoxalin-2-one, Bromodomain-containing protein 4 | | 著者 | Cao, D.Y, Li, Y.L, Du, Z.Y, Li, J, Xiong, B. | | 登録日 | 2019-02-20 | | 公開日 | 2020-02-26 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | brd4-bd1 bound with ligand 103
To Be Published
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8GPZ
 | | Crystal structure of BRD4 bromodomain 1 (BD1) in complex with C239-0012 | | 分子名称: | 3-methyl-6-(4-methylpiperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine, Bromodomain-containing protein 4, FORMIC ACID, ... | | 著者 | Park, T.H, Lee, B.I. | | 登録日 | 2022-08-27 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.528 Å) | | 主引用文献 | Crystal structure of [1,2,4]triazolo[4,3-b]pyridazine derivatives as BRD4 bromodomain inhibitors and structure-activity relationship study.
Sci Rep, 13, 2023
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8GQ0
 | | Crystal structure of BRD4 bromodomain 1 (BD1) in complex with STL233497 | | 分子名称: | Bromodomain-containing protein 4, FORMIC ACID, GLYCEROL, ... | | 著者 | Park, T.H, Lee, B.I. | | 登録日 | 2022-08-27 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.44 Å) | | 主引用文献 | Crystal structure of [1,2,4]triazolo[4,3-b]pyridazine derivatives as BRD4 bromodomain inhibitors and structure-activity relationship study.
Sci Rep, 13, 2023
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3JVJ
 | | Crystal structure of the bromodomain 1 in mouse Brd4 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, GLYCEROL | | 著者 | Vollmuth, F, Blankenfeldt, W, Geyer, M. | | 登録日 | 2009-09-17 | | 公開日 | 2009-10-13 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
J.Biol.Chem., 284, 2009
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4QR3
 | | Brd4 Bromodomain 1 complex with its novel inhibitors | | 分子名称: | Bromodomain-containing protein 4, N-cyclopentyl-3-(2-oxo-2,3-dihydro-1,3-thiazol-4-yl)benzenesulfonamide | | 著者 | Xiong, B, Cao, D.Y, Chen, T.T, Xu, Y.C. | | 登録日 | 2014-06-30 | | 公開日 | 2015-07-01 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (1.374 Å) | | 主引用文献 | Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization
J.Med.Chem., 58, 2015
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4QR4
 | | Brd4 Bromodomain 1 complex with its novel inhibitors | | 分子名称: | 2-chloro-N-cyclopentyl-5-(2-oxo-2,3-dihydro-1,3-thiazol-4-yl)benzenesulfonamide, Bromodomain-containing protein 4 | | 著者 | Xiong, B, Cao, D.Y, Chen, T.T, Xu, Y.C. | | 登録日 | 2014-06-30 | | 公開日 | 2015-07-01 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (1.28 Å) | | 主引用文献 | Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization
J.Med.Chem., 58, 2015
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3JVL
 | | Crystal structure of bromodomain 2 of mouse Brd4 | | 分子名称: | 1,2-ETHANEDIOL, BETA-MERCAPTOETHANOL, Bromodomain-containing protein 4 | | 著者 | Vollmuth, F, Blankenfeldt, W, Geyer, M. | | 登録日 | 2009-09-17 | | 公開日 | 2009-10-13 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
J.Biol.Chem., 284, 2009
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3JVM
 | | Crystal structure of bromodomain 2 of mouse Brd4 | | 分子名称: | 1,2-ETHANEDIOL, BETA-MERCAPTOETHANOL, Bromodomain-containing protein 4 | | 著者 | Vollmuth, F, Blankenfeldt, W, Geyer, M. | | 登録日 | 2009-09-17 | | 公開日 | 2009-10-13 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
J.Biol.Chem., 284, 2009
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3JVK
 | | Crystal structure of bromodomain 1 of mouse Brd4 in complex with histone H3-K(ac)14 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, histone H3.3 peptide | | 著者 | Vollmuth, F, Blankenfeldt, W, Geyer, M. | | 登録日 | 2009-09-17 | | 公開日 | 2009-10-13 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
J.Biol.Chem., 284, 2009
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5U2F
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5U2E
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7KHL
 | | BRD4-BD1 Compound6 (methyl 4-(3,5-difluoropyridin-2-yl)-10-methyl-7-((methylsulfonyl)methyl)-11-oxo-3,4,10,11-tetrahydro-1H-1,4,10-triazadibenzo[cd,f]azulene-6-carboxylate) | | 分子名称: | Bromodomain-containing protein 4, GLYCEROL, methyl 7-(3,5-difluoropyridin-2-yl)-2-methyl-10-[(methylsulfonyl)methyl]-3-oxo-3,4,6,7-tetrahydro-2H-2,4,7-triazadibenzo[cd,f]azulene-9-carboxylate | | 著者 | Murray, J.M. | | 登録日 | 2020-10-21 | | 公開日 | 2021-02-24 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.286 Å) | | 主引用文献 | Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
J.Med.Chem., 64, 2021
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7EHY
 | | BRD4-BD1 in complex with LT-448-138 | | 分子名称: | 1-[2,4-dimethyl-5-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-pyrrol-3-yl]ethanone, Bromodomain-containing protein 4 | | 著者 | Zheng, W, Kong, B, Tang, W, Zhu, J, Chen, Y. | | 登録日 | 2021-03-30 | | 公開日 | 2022-03-30 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.51 Å) | | 主引用文献 | BRD4-BD1 in complex with LT-642-602
To Be Published
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4DON
 | | Brd4 Bromodomain 1 complex with a fragment 3,4-Dihydro-3-methyl-2(1H)-quinazolinon | | 分子名称: | 3-methyl-3,4-dihydroquinazolin-2(1H)-one, Bromodomain-containing protein 4 | | 著者 | Xiong, B, Cao, D.Y, Chen, W.Y, Chen, T.T, Xu, Y.C, Shen, J.K. | | 登録日 | 2012-02-09 | | 公開日 | 2013-02-13 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (1.52 Å) | | 主引用文献 | Brd4 Bromodomain 1 complex with a fragment 3,4-Dihydro-3-methyl-2(1H)-quinazolinon
To be Published
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7EHW
 | | BRD4-BD1 in complex with LT-642-602 | | 分子名称: | 1-[4-ethyl-2-methyl-5-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-pyrrol-3-yl]ethanone, Bromodomain-containing protein 4 | | 著者 | Zheng, W, Kong, B, Tang, W, Zhu, J, Chen, Y. | | 登録日 | 2021-03-30 | | 公開日 | 2022-03-30 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | BRD4-BD1 in complex with LT-642-602
To Be Published
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7EIG
 | | BRD4-BD1 in complex with LT-730-903 | | 分子名称: | 1-[5-(5-azanyl-1H-benzimidazol-2-yl)-2-methyl-4-phenyl-1H-pyrrol-3-yl]ethanone, Bromodomain-containing protein 4 | | 著者 | Zheng, W, Kong, B, Tang, W, Zhu, J, Chen, Y. | | 登録日 | 2021-03-31 | | 公開日 | 2022-04-06 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.3 Å) | | 主引用文献 | BRD4-BD1 in complex with LT-730-903
To Be Published
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5I80
 | | BRD4 in complex with Cpd2 (N,N-dimethyl-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, DIMETHYL SULFOXIDE, ... | | 著者 | Murray, J.M. | | 登録日 | 2016-02-18 | | 公開日 | 2016-10-12 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.4501 Å) | | 主引用文献 | Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
J.Med.Chem., 59, 2016
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