4J3I
| X-ray crystal structure of bromodomain complex to 1.24 A resolution | Descriptor: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain-containing protein 4, ... | Authors: | Stein, A.J, White, A, Suto, R.K. | Deposit date: | 2013-02-05 | Release date: | 2014-01-15 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.24 Å) | Cite: | RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist. Plos One, 8, 2013
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4J0S
| Crystal Structure of the first bromodomain of human BRD4 in complex with a 3,5-dimethylisoxazol ligand | Descriptor: | 1,2-ETHANEDIOL, 3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(S)-hydroxy(phenyl)methyl]phenol, Bromodomain-containing protein 4 | Authors: | Filippakopoulos, P, Picaud, S, Qi, J, Felletar, I, Hewings, D.S, von Delft, F, Conway, S.J, Bountra, C, Arrowsmith, C.H, Edwards, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2013-01-31 | Release date: | 2013-02-13 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.84 Å) | Cite: | Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. J.Med.Chem., 56, 2013
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4J1P
| X-ray crystal structure of bromodomain 2 of human brd2 in complex with rvx208 to 1.08 A resolution | Descriptor: | 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, Bromodomain containing 2, ... | Authors: | Stein, A.J, White, A, Suto, R.K. | Deposit date: | 2013-02-01 | Release date: | 2014-01-15 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.08 Å) | Cite: | RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist. Plos One, 8, 2013
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4KCX
| BRDT in complex with Dinaciclib | Descriptor: | 3-[({3-ethyl-5-[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]pyrazolo[1,5-a]pyrimidin-7-yl}amino)methyl]-1-hydroxypyridinium, Bromodomain testis-specific protein, CHLORIDE ION | Authors: | Martin, M.P, Schonbrunn, E. | Deposit date: | 2013-04-24 | Release date: | 2013-09-18 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. Acs Chem.Biol., 8, 2013
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8E3W
| BRD4-D1 in complex with BET inhibitor | Descriptor: | (4P)-4-[2-(cyclopropylmethoxy)-5-(methanesulfonyl)phenyl]-2-methylisoquinolin-1(2H)-one, 1,2-ETHANEDIOL, Bromodomain-containing protein 4 | Authors: | Gorman, M.A, Fitzgerald, C.G.D, White, J.M, Parker, M.W. | Deposit date: | 2022-08-17 | Release date: | 2023-03-29 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.47 Å) | Cite: | Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission tomography. Chem.Commun.(Camb.), 59, 2023
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8E17
| BRD4-D1 in complex with BET inhibitor | Descriptor: | (4P,6M)-6-[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]-4-[5-(methanesulfonyl)-2-methoxyphenyl]-2-methylisoquinolin-1(2H)-one, 1,2-ETHANEDIOL, Bromodomain-containing protein 4 | Authors: | Gorman, M.A, Fitzgerald, C.G.D, White, J.M, Parker, M.W. | Deposit date: | 2022-08-09 | Release date: | 2023-03-29 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.47 Å) | Cite: | Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission tomography. Chem.Commun.(Camb.), 59, 2023
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8FTA
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8FVS
| Bromodomain of CBP liganded with CCS1477int | Descriptor: | 1,2-ETHANEDIOL, Histone acetyltransferase, MAGNESIUM ION, ... | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-19 | Release date: | 2024-01-24 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To Be Published
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8FV2
| Bromodomain of CBP liganded with CCS-1477 | Descriptor: | (6S)-1-[3,4-bis(fluoranyl)phenyl]-6-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-(4-methoxycyclohexyl)benzimidazol-2-yl]piperidin-2-one, 1,2-ETHANEDIOL, CREB-binding protein, ... | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-18 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.87 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To Be Published
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8FVK
| First bromodomain of BRD4 liganded with CCS-1477 | Descriptor: | (6S)-1-[3,4-bis(fluoranyl)phenyl]-6-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-(4-methoxycyclohexyl)benzimidazol-2-yl]piperidin-2-one, 1,2-ETHANEDIOL, Bromodomain-containing protein 4 | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-19 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.53 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To Be Published
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8FXA
| Bromodomain of CBP liganded with iCBP4 | Descriptor: | (6S)-1-[3,5-bis(trifluoromethyl)phenyl]-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, 1,2-ETHANEDIOL, CREB-binding protein | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-24 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To Be Published
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8FXO
| Bromodomain of CBP liganded with iCBP8 | Descriptor: | (6S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, CREB-binding protein | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-25 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.74 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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8FXE
| Bromodomain of CBP liganded with iCBP6 | Descriptor: | (6S)-1-(3-tert-butylphenyl)-6-{(5P)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, 1,2-ETHANEDIOL, CREB-binding protein | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-24 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.55 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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8FXN
| Bromodomain of CBP liganded with iCBP7 | Descriptor: | 1,2-ETHANEDIOL, CREB-binding protein, tert-butyl {(1R,4s)-4-[(5M)-2-[(2S)-1-(3-tert-butylphenyl)-6-oxopiperidin-2-yl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-benzimidazol-1-yl]cyclohexyl}carbamate | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-25 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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8G6T
| Bromodomain of CBP liganded with inhibitor iCBP2 | Descriptor: | (6S)-1-(3,4-dibromophenyl)-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}piperidin-2-one, CREB-binding protein, NICKEL (II) ION | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-02-15 | Release date: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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8FVF
| Bromodomain of EP300 liganded with CCS-1477 | Descriptor: | (6S)-1-[3,4-bis(fluoranyl)phenyl]-6-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-(4-methoxycyclohexyl)benzimidazol-2-yl]piperidin-2-one, 1,2-ETHANEDIOL, Histone acetyltransferase p300, ... | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-18 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To Be Published
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8FUP
| Bromodomain of CBP liganded with BMS-536924 and CCS-1477 | Descriptor: | (3M)-4-{[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(morpholin-4-yl)-1H-benzimidazol-2-yl]pyridin-2(1H)-one, (6S)-1-[3,4-bis(fluoranyl)phenyl]-6-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-(4-methoxycyclohexyl)benzimidazol-2-yl]piperidin-2-one, 1,2-ETHANEDIOL, ... | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-01-18 | Release date: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Structural basis of CBP and EP300 interaction with kinase inhibitors To Be Published
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8GA2
| Bromodomain of CBP liganded with inhibitor iCBP5 | Descriptor: | (6S)-6-{(5M)-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1s,4R)-4-methoxycyclohexyl]-1H-benzimidazol-2-yl}-1-phenylpiperidin-2-one, 1,2-ETHANEDIOL, CREB-binding protein | Authors: | Schonbrunn, E, Bikowitz, M. | Deposit date: | 2023-02-22 | Release date: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Group 3 medulloblastoma transcriptional networks are sensitive to EP300/CBP bromodomain inhibition To be published
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8GQ0
| Crystal structure of BRD4 bromodomain 1 (BD1) in complex with STL233497 | Descriptor: | Bromodomain-containing protein 4, FORMIC ACID, GLYCEROL, ... | Authors: | Park, T.H, Lee, B.I. | Deposit date: | 2022-08-27 | Release date: | 2023-01-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.44 Å) | Cite: | 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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8GPZ
| Crystal structure of BRD4 bromodomain 1 (BD1) in complex with C239-0012 | Descriptor: | 3-methyl-6-(4-methylpiperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine, Bromodomain-containing protein 4, FORMIC ACID, ... | Authors: | Park, T.H, Lee, B.I. | Deposit date: | 2022-08-27 | Release date: | 2023-01-18 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.528 Å) | Cite: | 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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3ZYU
| Crystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A) | Descriptor: | 1,2-ETHANEDIOL, 7-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-8-METHOXY-1-[(1R)-1-(PYRIDIN-2-YL)ETHYL]-1H,2H,3H-IMIDAZO[4,5-C]QUINOLIN-2-ONE, BROMODOMAIN-CONTAINING PROTEIN 4 | Authors: | Chung, C.W, Mirguet, O. | Deposit date: | 2011-08-25 | Release date: | 2011-11-02 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Inhibition of Bet Recruitment to Chromatin as an Effective Treatment for Mll-Fusion Leukaemia. Nature, 478, 2011
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4A9E
| N-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 3-methyl-1,2,3,4- tetrahydroquinazolin-2-one | Descriptor: | 1,2-ETHANEDIOL, 3-methyl-3,4-dihydroquinazolin-2(1H)-one, BROMODOMAIN-CONTAINING PROTEIN 2, ... | Authors: | Chung, C, Bamborough, P. | Deposit date: | 2011-11-26 | Release date: | 2012-01-11 | Last modified: | 2019-05-08 | Method: | X-RAY DIFFRACTION (1.91 Å) | Cite: | Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery. J.Med.Chem., 55, 2012
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4A9J
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7S3P
| BD2 domain of human BRD3 bound to Physachenolide C | Descriptor: | Bromodomain-containing protein 3, CHLORIDE ION, Physachenolide C | Authors: | Horton, N.C, Chapman, E, Sivinski, J, Zerio, C, Ghadirian, N. | Deposit date: | 2021-09-07 | Release date: | 2023-01-11 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (2.89 Å) | Cite: | Physachenolide C is a Potent, Selective BET Inhibitor. J.Med.Chem., 66, 2023
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4A9M
| N-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-cyclopentyl-5-(3,5- dimethyl-1,2-oxazol-4-yl)-2-methylbenzene-1-sulfonamide | Descriptor: | BROMODOMAIN CONTAINING 2, N-cyclopentyl-5-(3,5-dimethylisoxazol-4-yl)-2-methylbenzenesulfonamide, SULFATE ION | Authors: | Chung, C, Bamborough, P. | Deposit date: | 2011-11-26 | Release date: | 2012-02-08 | Method: | X-RAY DIFFRACTION (2.06 Å) | Cite: | Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides. J.Med.Chem., 55, 2012
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