6FS0
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3ZMM
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![BU of 3zmm by Molmil](/molmil-images/mine/3zmm) | Inhibitors of Jak2 Kinase domain | 分子名称: | 5-FLUORO-4-[(1S)-1-(5-FLUOROPYRIMIDIN-2-YL)ETHOXY]-N-(5-METHYL-1H-PYRAZOL-3-YL)-6-MORPHOLINO-PYRIMIDIN-2-AMINE, ACETYL GROUP, TYROSINE-PROTEIN KINASE JAK2 | 著者 | Read, J, Green, I, Pollard, H, Howard, T, Mott, R. | 登録日 | 2013-02-11 | 公開日 | 2013-04-17 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.51 Å) | 主引用文献 | Discovery of Novel Jak2-Stat Pathway Inhibitors with Extended Residence Time on Target. Bioorg.Med.Chem.Lett., 23, 2013
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4DTK
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![BU of 4dtk by Molmil](/molmil-images/mine/4dtk) | Novel and selective pan-PIM kinase inhibitor | 分子名称: | (5Z)-5-{2-[(3R)-3-aminopiperidin-1-yl]-3-(propan-2-yloxy)benzylidene}-1,3-thiazolidine-2,4-dione, 1,2-ETHANEDIOL, SULFATE ION, ... | 著者 | Ferguson, A.D. | 登録日 | 2012-02-21 | 公開日 | 2012-07-11 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.86 Å) | 主引用文献 | Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg.Med.Chem.Lett., 22, 2012
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8RPO
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![BU of 8rpo by Molmil](/molmil-images/mine/8rpo) | BFL1 in complex with a reversible covalent ligand | 分子名称: | (~{E})-2-cyano-3-(2-dimethylphosphorylphenyl)-~{N}-[[1-[4-(trifluoromethyl)phenyl]cyclopropyl]methyl]prop-2-enamide, Bcl-2-related protein A1 | 著者 | Hargreaves, D. | 登録日 | 2024-01-16 | 公開日 | 2024-07-03 | 実験手法 | X-RAY DIFFRACTION (1.791 Å) | 主引用文献 | Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen. Acs Med.Chem.Lett., 15, 2024
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8QTG
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![BU of 8qtg by Molmil](/molmil-images/mine/8qtg) | Crystal structure of CBL-b in complex with an allosteric inhibitor (compound 9) | 分子名称: | 3-[3-[3-methyl-1-(4-methyl-1,2,4-triazol-3-yl)cyclobutyl]phenyl]-5-(trifluoromethyl)-1~{H}-pyridin-2-one, E3 ubiquitin-protein ligase CBL-B, SODIUM ION, ... | 著者 | Schimpl, M. | 登録日 | 2023-10-12 | 公開日 | 2024-01-10 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.419 Å) | 主引用文献 | Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors. J.Med.Chem., 67, 2024
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8QTH
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![BU of 8qth by Molmil](/molmil-images/mine/8qth) | Crystal structure of CBL-b in complex with an allosteric inhibitor (compound 8) | 分子名称: | 1-methyl-5-[3-[3-methyl-1-(4-methyl-1,2,4-triazol-3-yl)cyclobutyl]phenyl]-3-(trifluoromethyl)-7H-pyrrolo[2,3-b]pyridin-6-one, E3 ubiquitin-protein ligase CBL-B, SODIUM ION, ... | 著者 | Schimpl, M. | 登録日 | 2023-10-12 | 公開日 | 2024-01-10 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2.198 Å) | 主引用文献 | Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors. J.Med.Chem., 67, 2024
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8QTJ
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![BU of 8qtj by Molmil](/molmil-images/mine/8qtj) | Crystal structure of Cbl-b in complex with an allosteric inhibitor (compound 30) | 分子名称: | 3-[3-[3-methyl-1-(4-methyl-1,2,4-triazol-3-yl)cyclobutyl]phenyl]-1-[(1~{R})-1-(1-methylpyrazol-4-yl)ethyl]-5-(trifluoromethyl)pyridin-2-one, E3 ubiquitin-protein ligase CBL-B, SODIUM ION, ... | 著者 | Schimpl, M. | 登録日 | 2023-10-12 | 公開日 | 2024-01-10 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.523 Å) | 主引用文献 | Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors. J.Med.Chem., 67, 2024
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8QTK
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![BU of 8qtk by Molmil](/molmil-images/mine/8qtk) | Crystal structure of CBL-b in complex with an allosteric inhibitor (compound 31) | 分子名称: | 3-[3-[3-methyl-1-(4-methyl-1,2,4-triazol-3-yl)cyclobutyl]phenyl]-1-[(1S)-1-(1-methylpyrazol-4-yl)ethyl]-5-(trifluoromethyl)pyridin-2-one, E3 ubiquitin-protein ligase CBL-B, SODIUM ION, ... | 著者 | Schimpl, M. | 登録日 | 2023-10-12 | 公開日 | 2024-01-24 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.873 Å) | 主引用文献 | Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors. J.Med.Chem., 67, 2024
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4C61
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![BU of 4c61 by Molmil](/molmil-images/mine/4c61) | Inhibitors of Jak2 Kinase domain | 分子名称: | ACETATE ION, N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-7-methyl-N4-(1-methylimidazol-4-yl)thieno[3,2-d]pyrimidine-2,4-diamine, TYROSINE-PROTEIN KINASE JAK2 | 著者 | Read, J.A, Green, I, Pollard, H, Howard, T. | 登録日 | 2013-09-17 | 公開日 | 2014-01-08 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | 主引用文献 | Discovery of 1-Methyl-1H-Imidazole Derivatives as Potent Jak2 Inhibitors. J.Med.Chem., 57, 2014
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4C62
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![BU of 4c62 by Molmil](/molmil-images/mine/4c62) | Inhibitors of Jak2 Kinase domain | 分子名称: | ACETATE ION, N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-n4-(1-methylimidazol-4-yl)-6-morpholino-1,3,5-triazine-2,4-diamine, TYROSINE-PROTEIN KINASE JAK2 | 著者 | Read, J, Green, I, Pollard, H, Howard, T. | 登録日 | 2013-09-17 | 公開日 | 2014-01-08 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | 主引用文献 | Discovery of 1-Methyl-1H-Imidazole Derivatives as Potent Jak2 Inhibitors. J.Med.Chem., 57, 2014
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