3U5L
 
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a benzo-triazepine ligand (BzT-7) | | 分子名称: | 1,2-ETHANEDIOL, 8-chloro-1,4-dimethyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,3,4]benzotriazepine, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Bracher, F, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-10-11 | | 公開日 | 2011-11-23 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.39 Å) | | 主引用文献 | Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Bioorg.Med.Chem., 20, 2012
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3U5K
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with Midazolam | | 分子名称: | 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine, Bromodomain-containing protein 4 | | 著者 | Filippakopoulos, P, Picaud, S, Felletar, I, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-10-11 | | 公開日 | 2011-11-23 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Bioorg.Med.Chem., 20, 2012
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5BT5
 | | Crystal structure of BRD2 second bromodomain in complex with SGC-CBP30 chemical probe | | 分子名称: | 1,2-ETHANEDIOL, 2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-benzimidazole, Bromodomain-containing protein 2 | | 著者 | Tallant, C, Hay, D, Krojer, T, Nunez-Alonso, G, Picaud, S, Newman, J.A, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Brennan, P.E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2015-06-02 | | 公開日 | 2015-07-01 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | Crystal structure of BRD2 second bromodomain in complex with a 3,5-dimethylisoxazol ligand
To Be Published
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5BT3
 | | Crystal structure of EP300 bromodomain in complex with SGC-CBP30 chemical probe | | 分子名称: | 2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-benzimidazole, Histone acetyltransferase p300, ISOPROPYL ALCOHOL | | 著者 | Tallant, C, Hay, D, Krojer, T, Nunez-Alonso, G, Picaud, S, Newman, J.A, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Brennan, P.E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2015-06-02 | | 公開日 | 2015-07-01 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.05 Å) | | 主引用文献 | Crystal structure of EP300 bromodomain in complex with a 3,5-dimethylisoxazol ligand
To Be Published
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2GJT
 | | Crystal structure of the human receptor phosphatase PTPRO | | 分子名称: | CHLORIDE ION, Receptor-type tyrosine-protein phosphatase PTPRO | | 著者 | Barr, A, Ugochukwu, E, Eswaran, J, Das, S, Niesen, F, Savitsky, P, Turnbull, A, Sundstrom, M, Arrowsmith, C, Edwards, A, Weigelt, J, von Delft, F, Papagrigoriou, E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2006-03-31 | | 公開日 | 2006-05-02 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | Large-scale structural analysis of the classical human protein tyrosine phosphatome.
Cell(Cambridge,Mass.), 136, 2009
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3UV2
 | | Crystal structure of the bromodomain of human nucleosome-remodeling factor subunit BPTF | | 分子名称: | 2-(2-(2-(2-(2-(2-ETHOXYETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHANOL, bromodomain of human nucleosome-remodeling factor subunit BPTF | | 著者 | Filippakopoulos, P, Picaud, S, Keates, T, Ugochukwu, E, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-29 | | 公開日 | 2012-01-18 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.58 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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3UVW
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H4K5acK8ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, Histone H4 | | 著者 | Filippakopoulos, P, Felletar, I, Picaud, S, Keates, T, Muniz, J, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-30 | | 公開日 | 2012-01-18 | | 最終更新日 | 2023-12-06 | | 実験手法 | X-RAY DIFFRACTION (1.37 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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3UW9
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H4K8acK12ac) | | 分子名称: | Bromodomain-containing protein 4, histone 4 peptide (H4K8acK12ac) | | 著者 | Filippakopoulos, P, Felletar, I, Picaud, S, Keates, T, Muniz, J, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-12-01 | | 公開日 | 2012-03-14 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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3UV5
 | | Crystal Structure of the tandem bromodomains of human Transcription initiation factor TFIID subunit 1 (TAF1) | | 分子名称: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Transcription initiation factor TFIID subunit 1 | | 著者 | Filippakopoulos, P, Felletar, I, Picaud, S, Keates, T, Muniz, J, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-29 | | 公開日 | 2012-01-18 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.03 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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3UVY
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H4K16acK20ac) | | 分子名称: | Bromodomain-containing protein 4, Histone H4 | | 著者 | Filippakopoulos, P, Felletar, I, Picaud, S, Keates, T, Muniz, J, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-30 | | 公開日 | 2012-01-18 | | 最終更新日 | 2023-12-06 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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4CRS
 | | Human Protein Kinase N2 (PKN2, PRKCL2) in complex with ATPgammaS | | 分子名称: | MAGNESIUM ION, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, SERINE/THREONINE-PROTEIN KINASE N2, ... | | 著者 | Mathea, S, Elkins, J.M, Shrestha, L, Szklarz, M, Tallant, C, Newman, J.A, Cooper, C.D, Shrestha, B, Tumber, A, Cocking, R, Salah, E, von Delft, F, Arrowsmith, C, Edwards, A.M, Bountra, C, Knapp, S. | | 登録日 | 2014-02-28 | | 公開日 | 2014-03-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | | 主引用文献 | Structure of Pkn2
To be Published
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4LC2
 | | Crystal structure of the bromodomain of human BRPF1B | | 分子名称: | 1,2-ETHANEDIOL, NITRATE ION, Peregrin | | 著者 | Tallant, C, Nunez-Alonso, G, Savitsky, P, Picaud, S, Filippakopoulos, P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2013-06-21 | | 公開日 | 2013-07-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Crystal structure of the bromodomain of human BRPF1B
TO BE PUBLISHED
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5E9V
 | | Crystal structure of BRD9 bromodomain in complex with an indolizine ligand | | 分子名称: | 1,2-ETHANEDIOL, 1-[1-(imidazo[1,2-a]pyridin-5-yl)-7-(morpholin-4-yl)indolizin-3-yl]ethanone, Bromodomain-containing protein 9 | | 著者 | Tallant, C, Hay, D.A, Krojer, T, Nunez-Alonso, G, Picaud, S, Fedorov, O, Schofield, C.J, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Brennan, P.E, Knapp, S. | | 登録日 | 2015-10-15 | | 公開日 | 2015-10-28 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Crystal structure of BRD9 bromodomain in complex with an indolizine ligand
To Be Published
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6HT1
 | | Crystal structure of MLLT1 (ENL) YEATS domain in complexed with SGC-iMLLT (compound 92) | | 分子名称: | 1,2-ETHANEDIOL, 1-methyl-~{N}-[2-[[(2~{S})-2-methylpyrrolidin-1-yl]methyl]-3~{H}-benzimidazol-5-yl]indazole-5-carboxamide, Protein ENL, ... | | 著者 | Heidenreich, D, Chaikuad, A, Moustakim, M, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Fedorov, O, Brennan, P.E, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2018-10-02 | | 公開日 | 2018-10-17 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery of an MLLT1/3 YEATS Domain Chemical Probe.
Angew. Chem. Int. Ed. Engl., 57, 2018
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6HDR
 | | Human DYRK2 bound to Curcumin | | 分子名称: | DITHIANE DIOL, Dual specificity tyrosine-phosphorylation-regulated kinase 2, PHOSPHATE ION, ... | | 著者 | Elkins, J.M, Soundararajan, M, Vollmar, M, Krojer, T, Bountra, C, Edwards, A.M, Arrowsmith, C, Knapp, S. | | 登録日 | 2018-08-18 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | DYRK2 bound to Curcumin
To Be Published
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6HDP
 | | Human DYRK2 bound to Scorzodihydrostilbene A | | 分子名称: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, SODIUM ION, Scorzodihydrostilbene A | | 著者 | Elkins, J.M, Soundararajan, M, Proksch, P, Meijer, L, Vollmar, M, Krojer, T, Bountra, C, Edwards, A.M, Arrowsmith, C, Knapp, S. | | 登録日 | 2018-08-18 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | DYRK2 bound to Scorzodihydrostilbene A
To Be Published
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3UVX
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with a diacetylated histone 4 peptide (H4K12acK16ac) | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, FORMIC ACID, ... | | 著者 | Filippakopoulos, P, Picaud, S, Keates, T, Ugochukwu, E, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2011-11-30 | | 公開日 | 2012-01-25 | | 最終更新日 | 2023-12-06 | | 実験手法 | X-RAY DIFFRACTION (1.91 Å) | | 主引用文献 | Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell(Cambridge,Mass.), 149, 2012
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2JJD
 | | Protein Tyrosine Phosphatase, Receptor Type, E isoform | | 分子名称: | CHLORIDE ION, RECEPTOR-TYPE TYROSINE-PROTEIN PHOSPHATASE EPSILON | | 著者 | Elkins, J.M, Ugochukwu, E, Alfano, I, Barr, A.J, Bunkoczi, G, King, O.N.F, Filippakopoulos, P, Savitsky, P, Salah, E, Pike, A, Johansson, C, Das, S, Burgess-Brown, N.A, Gileadi, O, von Delft, F, Arrowsmith, C.H, Bountra, C, Edwards, A.M, Knapp, S. | | 登録日 | 2008-03-31 | | 公開日 | 2008-04-08 | | 最終更新日 | 2012-06-06 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Large-Scale Structural Analysis of the Classical Human Protein Tyrosine Phosphatome.
Cell(Cambridge,Mass.), 136, 2009
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8P9L
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB512 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-azanyl-5-phenyl-phenyl)-5-(6-methyl-7-oxidanylidene-1~{H}-pyrrolo[2,3-c]pyridin-4-yl)pyridine-2-carboxamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.29 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB512
to be published
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8P9G
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB390 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-aminophenyl)-4-[(~{E})-(6-methyl-7-oxidanyl-1~{H}-indol-4-yl)diazenyl]benzamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.1 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB390
to be published
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8P9I
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB462 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-aminophenyl)-4-(6-methyl-7-oxidanylidene-1~{H}-pyrrolo[2,3-c]pyridin-4-yl)benzamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.23 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB462
to be published
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8P9J
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB500 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-aminophenyl)-5-(6-methyl-7-oxidanylidene-1~{H}-pyrrolo[2,3-c]pyridin-4-yl)pyridine-2-carboxamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.42 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB500
to be published
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8P9K
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB503 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-azanyl-5-phenyl-phenyl)-4-(6-methyl-7-oxidanylidene-1~{H}-pyrrolo[2,3-c]pyridin-4-yl)benzamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.25 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB503
to be published
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8P9F
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB161 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-aminophenyl)-4-[2-(2-azanyl-5-methyl-4-oxidanyl-phenyl)hydrazinyl]benzamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.3 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB161
to be published
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8P9H
 | | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB437 | | 分子名称: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, ~{N}-(2-aminophenyl)-2-(6-methyl-7-oxidanylidene-1~{H}-pyrrolo[2,3-c]pyridin-4-yl)quinoline-6-carboxamide | | 著者 | Balourdas, D.I, Bauer, N, Knapp, S, Joerger, A.C, Structural Genomics Consortium (SGC) | | 登録日 | 2023-06-06 | | 公開日 | 2023-07-05 | | 実験手法 | X-RAY DIFFRACTION (1.19 Å) | | 主引用文献 | Crystal structure of the first bromodomain of human BRD4 in complex with the dual BET/HDAC inhibitor NB437
to be published
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