3O36
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3O35
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3O33
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3O34
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3O37
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5H1U
| Complex structure of TRIM24 PHD-bromodomain and inhibitor 2 | Descriptor: | 2-amino-1,3-benzothiazole-6-carboxamide, DIMETHYL SULFOXIDE, Transcription intermediary factor 1-alpha, ... | Authors: | Liu, J. | Deposit date: | 2016-10-11 | Release date: | 2017-02-22 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.901 Å) | Cite: | The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network FEBS J., 284, 2017
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5H1T
| Complex structure of TRIM24 PHD-bromodomain and inhibitor 1 | Descriptor: | DIMETHYL SULFOXIDE, Transcription intermediary factor 1-alpha, ZINC ION, ... | Authors: | Liu, J. | Deposit date: | 2016-10-11 | Release date: | 2017-02-22 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.951 Å) | Cite: | The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network FEBS J., 284, 2017
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5H1V
| Complex structure of TRIM24 PHD-bromodomain and inhibitor 6 | Descriptor: | 2-Hydrazino-1,3-benzothiazole-6-carbohydrazide, DIMETHYL SULFOXIDE, Transcription intermediary factor 1-alpha, ... | Authors: | Liu, J. | Deposit date: | 2016-10-11 | Release date: | 2017-02-22 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.002 Å) | Cite: | The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network FEBS J., 284, 2017
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7B9X
| NMR2 structure of TRIM24-BD in complex with a precursor of IACS-9571 | Descriptor: | N-{6-[3-(4-Aminobutoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl}-3,4-dimethoxybenzene-1-sulfonamide, Transcription intermediary factor 1-alpha | Authors: | Orts, J, Torres, F, Milbradt, A.G, Walser, R. | Deposit date: | 2020-12-14 | Release date: | 2022-01-12 | Last modified: | 2022-04-27 | Method: | SOLUTION NMR | Cite: | NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24. J.Med.Chem., 65, 2022
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4YC9
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-(6-{3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy}-1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl)-3,4-dimethoxybenzene-1-sulfonamide (8i) | Descriptor: | GLYCEROL, N-(6-{3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy}-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)-3,4-dimethoxybenzenesulfonamide, Transcription intermediary factor 1-alpha, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-19 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.82 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YAB
| Crystal structure of TRIM24 PHD-bromodomain complexed with 1-methyl-5-(2-methyl-1 3-thiazol-4-yl)-2 3-dihydro-1H-indol-2-one (1) | Descriptor: | 1-methyl-5-(2-methyl-1,3-thiazol-4-yl)-1,3-dihydro-2H-indol-2-one, SULFATE ION, Transcription intermediary factor 1-alpha, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-17 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YAD
| Crystal structure of TRIM24 PHD-bromodomain complexed with 2,4-dimethoxy-N-(1-methyl-2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)benzene-1-sulfonamide (3b) | Descriptor: | 2,4-dimethoxy-N-(1-methyl-2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)benzenesulfonamide, CHLORIDE ION, GLYCEROL, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-17 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.73 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YBM
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-{6-[3-(benzyloxy)phenoxy]-1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl}-3,4-dimethoxybenzene-1-sulfonamide (7b) | Descriptor: | GLYCEROL, N-{6-[3-(benzyloxy)phenoxy]-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl}-3,4-dimethoxybenzenesulfonamide, SULFATE ION, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-18 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.46 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YBS
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-{1,3-dimethyl-6-[3-(2-methylpropoxy)phenoxy]-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl}-1,2-dimethyl-1H-imidazole-4-sulfonamide (7g) | Descriptor: | DIMETHYL SULFOXIDE, N-{1,3-dimethyl-6-[3-(2-methylpropoxy)phenoxy]-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl}-1,2-dimethyl-1H-imidazole-4-sulfonamide, Transcription intermediary factor 1-alpha, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-19 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.83 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YAT
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-(1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl)-4-methoxybenzene-1-sulfonamide (5b) | Descriptor: | N-(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)-4-methoxybenzenesulfonamide, Transcription intermediary factor 1-alpha, ZINC ION | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-17 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.18 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YBT
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-{1,3-dimethyl-2-oxo-6-[3-(oxolan-3-ylmethoxy)phenoxy]-2,3-dihydro-1H-1,3-benzodiazol-5-yl}-1-methyl-1H-imidazole-4-sulfonamide (7l) | Descriptor: | DIMETHYL SULFOXIDE, N-(1,3-dimethyl-2-oxo-6-{3-[(3S)-tetrahydrofuran-3-ylmethoxy]phenoxy}-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-imidazole-4-sulfonamide, Transcription intermediary factor 1-alpha, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-19 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.82 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4YAX
| Crystal structure of TRIM24 PHD-bromodomain complexed with N-[6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl]benzenesulfonamide (5g) | Descriptor: | GLYCEROL, N-[6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl]benzenesulfonamide, SULFATE ION, ... | Authors: | Poncet-Montange, G, Palmer, W, Jones, P. | Deposit date: | 2015-02-18 | Release date: | 2015-06-24 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.25 Å) | Cite: | Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J.Med.Chem., 59, 2016
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4ZQL
| Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor | Descriptor: | 3,4-dimethoxy-N-[6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl]benzenesulfonamide, DIMETHYL SULFOXIDE, PENTAETHYLENE GLYCOL, ... | Authors: | Tallant, C, Structural Genomics Consortium (SGC), Clark, P.G.K, Vieira, L.C.C, Krojer, T, Nunez-Alonso, G, Picaud, S, Fedorov, O, Dixon, D.J, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Brennan, P.E, Knapp, S. | Deposit date: | 2015-05-10 | Release date: | 2015-06-17 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (1.79 Å) | Cite: | Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor To Be Published
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7AQT
| NMR2 structure of BRD4-BD2 in complex with iBET-762 | Descriptor: | 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide, Bromodomain-containing protein 4 | Authors: | Orts, J, Torres, F, Milbradt, A.G, Walser, R. | Deposit date: | 2020-10-23 | Release date: | 2022-03-02 | Last modified: | 2022-04-27 | Method: | SOLUTION NMR | Cite: | NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24. J.Med.Chem., 65, 2022
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8BDY
| Crystal structure of TRIM33 alpha PHD-Bromo domain in complex with 9 | Descriptor: | 1,3-dimethylbenzimidazol-2-one, CALCIUM ION, E3 ubiquitin-protein ligase TRIM33, ... | Authors: | Tassone, G, Pozzi, C, Palomba, T. | Deposit date: | 2022-10-20 | Release date: | 2022-12-07 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.05 Å) | Cite: | Exploiting ELIOT for Scaffold-Repurposing Opportunities: TRIM33 a Possible Novel E3 Ligase to Expand the Toolbox for PROTAC Design. Int J Mol Sci, 23, 2022
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8BD8
| Crystal structure of TRIM33 alpha PHD-Bromo domain in complex with 8 | Descriptor: | 1,3-dimethylbenzimidazol-2-one, CALCIUM ION, E3 ubiquitin-protein ligase TRIM33, ... | Authors: | Tassone, G, Pozzi, C, Palomba, T. | Deposit date: | 2022-10-18 | Release date: | 2022-12-07 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.1 Å) | Cite: | Exploiting ELIOT for Scaffold-Repurposing Opportunities: TRIM33 a Possible Novel E3 Ligase to Expand the Toolbox for PROTAC Design. Int J Mol Sci, 23, 2022
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8BD9
| Crystal structure of TRIM33 alpha PHD-Bromo domain in complex with 10 | Descriptor: | 1,3-dimethylbenzimidazol-2-one, CALCIUM ION, E3 ubiquitin-protein ligase TRIM33, ... | Authors: | Tassone, G, Pozzi, C, Palomba, T. | Deposit date: | 2022-10-18 | Release date: | 2022-12-07 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Exploiting ELIOT for Scaffold-Repurposing Opportunities: TRIM33 a Possible Novel E3 Ligase to Expand the Toolbox for PROTAC Design. Int J Mol Sci, 23, 2022
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7RUN
| Crystal structure of phosphorylated RET tyrosine kinase domain complexed with a pyrrolo[2,3-d]pyrimidine inhibitor. | Descriptor: | 1-(4-{(1s,3s)-3-[4-amino-5-(3-amino-4-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl}piperazin-1-yl)ethan-1-one, CHLORIDE ION, Proto-oncogene tyrosine-protein kinase receptor Ret | Authors: | Lee, C.C, Spraggon, G. | Deposit date: | 2021-08-17 | Release date: | 2022-01-19 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (3.51 Å) | Cite: | Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3- d ]pyrimidine RET Inhibitors. Acs Med.Chem.Lett., 12, 2021
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6VHG
| Crystal structure of phosphorylated RET tyrosine kinase domain complexed with a pyrazolo[1,5-a]pyrimidine inhibitor | Descriptor: | 3-(3,4-dimethoxyphenyl)-N~5~-(1-methylpiperidin-4-yl)-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine, ACETATE ION, CHLORIDE ION, ... | Authors: | Lee, C.C, Spraggon, G. | Deposit date: | 2020-01-09 | Release date: | 2020-02-26 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.303 Å) | Cite: | Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. Acs Med.Chem.Lett., 11, 2020
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6FEK
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