6YQR
 
 | | BRD9 with Biphenyl-methylamino-dimethylpyridazinone | | Descriptor: | 2,4-dimethyl-5-[(2-phenylphenyl)methylamino]pyridazin-3-one, Bromodomain-containing protein 9 | | Authors: | Chung, C. | | Deposit date: | 2020-04-18 | | Release date: | 2021-03-24 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.684 Å) | | Cite: | Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
J.Med.Chem., 63, 2020
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6YQZ
 | | N-terminal domain of BRD4 with biphenyl-methyamino-dimethylpyridazinone | | Descriptor: | 1,2-ETHANEDIOL, 2,4-dimethyl-5-[(2-phenylphenyl)methylamino]pyridazin-3-one, Bromodomain-containing protein 4 | | Authors: | Chung, C. | | Deposit date: | 2020-04-18 | | Release date: | 2021-03-24 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.39 Å) | | Cite: | Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
J.Med.Chem., 63, 2020
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6YQW
 | | BRD9 with 4-chloro-2-methyl-methylamino-pyridazinone | | Descriptor: | 4-chloranyl-2-methyl-5-(methylamino)pyridazin-3-one, Bromodomain-containing protein 9 | | Authors: | Chung, C. | | Deposit date: | 2020-04-18 | | Release date: | 2021-04-14 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
J.Med.Chem., 63, 2020
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6Z7G
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6ZB1
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK620 | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, ~{N}5-cyclopropyl-~{N}3-methyl-2-oxidanylidene-1-(phenylmethyl)pyridine-3,5-dicarboxamide | | Authors: | Chung, C. | | Deposit date: | 2020-06-06 | | Release date: | 2020-08-05 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
J.Med.Chem., 63, 2020
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6Z7F
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6ZB3
 | | N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH GSK620 | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, PENTAETHYLENE GLYCOL, ... | | Authors: | Chung, C. | | Deposit date: | 2020-06-06 | | Release date: | 2020-08-05 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.419 Å) | | Cite: | The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
J.Med.Chem., 63, 2020
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6ZB2
 | | C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK549 | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 2, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Chung, C. | | Deposit date: | 2020-06-06 | | Release date: | 2020-08-05 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.282 Å) | | Cite: | The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
J.Med.Chem., 63, 2020
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6ZB0
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7A9U
 | | N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 3-(3-(but-3-yn-1-yl)-3H-diazirin-3-yl)-N-(3-methyl-[1,2,4]triazolo[4,3-a]pyridin-8-yl)propanamide | | Descriptor: | 1,2-ETHANEDIOL, 3-(3-(but-3-yn-1-yl)-3H-diazirin-3-yl)-N-(3-methyl-[1,2,4]triazolo[4,3-a]pyridin-8-yl)propanamide, Bromodomain-containing protein 4 | | Authors: | Chung, C. | | Deposit date: | 2020-09-02 | | Release date: | 2020-10-21 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (1.444 Å) | | Cite: | A Photoaffinity-Based Fragment-Screening Platform for Efficient Identification of Protein Ligands.
Angew.Chem.Int.Ed.Engl., 59, 2020
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4C67
 | | Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains | | Descriptor: | 1,2-ETHANEDIOL, 13-methyl-7-phenyl-3-thia-1,8,11,12-tetraazatricyclo trideca-2(6),4,7,10,12-pentaene, BROMODOMAIN-CONTAINING PROTEIN 4 | | Authors: | Chung, C, Mirguet, O. | | Deposit date: | 2013-09-17 | | Release date: | 2013-10-02 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Discovery of Epigenetic Regulator I-Bet762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the Bet Bromodomains.
J.Med.Chem., 56, 2013
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6YB4
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4ALG
 | | N-Terminal Bromodomain of Human BRD2 With IBET-151 | | Descriptor: | 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, ACETATE ION, BROMODOMAIN-CONTAINING PROTEIN 2, ... | | Authors: | Chung, C, Lamotte, Y, Donche, F, Bouillot, A, Mirguet, O. | | Deposit date: | 2012-03-03 | | Release date: | 2012-07-04 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Identification of a Novel Series of Bet Family Bromodomain Inhibitors: Binding Mode and Profile of I-Bet151 (Gsk1210151A).
Bioorg.Med.Chem.Lett., 22, 2012
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4AKN
 | | N-Terminal Bromodomain of Human BRD2 With tbutyl-phenyl-amino- dimethyl-oxazolyl-quinoline-carboxylic acid | | Descriptor: | 1,2-ETHANEDIOL, 4-[(2-tert-butylphenyl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)quinoline-3-carboxylic acid, BROMODOMAIN-CONTAINING PROTEIN 2, ... | | Authors: | Chung, C, Lamotte, Y, Donche, F, Bouillot, A, Mirguet, O. | | Deposit date: | 2012-02-26 | | Release date: | 2012-07-04 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.82 Å) | | Cite: | Identification of a Novel Series of Bet Family Bromodomain Inhibitors: Binding Mode and Profile of I-Bet151 (Gsk1210151A).
Bioorg.Med.Chem.Lett., 22, 2012
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