8GMC
| CRYSTAL STRUCTURE OF AP2 ASSOCIATED KINASE 1 COMPLEXED WITH 5-[(4-aminopiperidin-1-yl)methyl]-N-{3-[5-(propan-2-yl)-1,3,4-thiadiazol-2-yl]phenyl}pyrrolo[2,1-f][1,2,4]triazin-4-amine | 分子名称: | 5-[(4-aminopiperidin-1-yl)methyl]-N-{3-[5-(propan-2-yl)-1,3,4-thiadiazol-2-yl]phenyl}pyrrolo[2,1-f][1,2,4]triazin-4-amine, AP2-associated protein kinase 1, SULFATE ION | 著者 | Muckelbauer, J.K. | 登録日 | 2023-03-24 | 公開日 | 2023-07-12 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Discovery of pyrrolo[2,1- f ][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain. Med.Chem.Res., 2023
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8GMD
| CRYSTAL STRUCTURE OF AP2 ASSOCIATED KINASE 1 COMPLEXED WITH (5P)-3-({(8R)-5-[(4-aminopiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}amino)-5-[2-(propan-2-yl)-2H-tetrazol-5-yl]phenol | 分子名称: | (5P)-3-({(8R)-5-[(4-aminopiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}amino)-5-[2-(propan-2-yl)-2H-tetrazol-5-yl]phenol, AP2-associated protein kinase 1, SULFATE ION | 著者 | Muckelbauer, J.K. | 登録日 | 2023-03-24 | 公開日 | 2023-07-12 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Discovery of pyrrolo[2,1- f ][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain. Med.Chem.Res., 2023
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8H59
| A fungal MAP kinase in complex with an inhibitor | 分子名称: | Mitogen-activated protein kinase MPS1, ~{N}-[(2~{S})-3-(1~{H}-indol-3-yl)-1-(methylamino)-1-oxidanylidene-propan-2-yl]-8-[2-methoxy-5-(trifluoromethyloxy)phenyl]-1,6-naphthyridine-2-carboxamide | 著者 | Kong, Z, Zhang, X, Wang, D, Liu, J. | 登録日 | 2022-10-12 | 公開日 | 2023-02-08 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | Structure-Aided Identification of an Inhibitor Targets Mps1 for the Management of Plant-Pathogenic Fungi. Mbio, 14, 2023
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8HLT
| The co-crystal structure of DYRK2 with YK-2-99B | 分子名称: | (6-{[(4P)-4-(1,3-benzothiazol-5-yl)-5-fluoropyrimidin-2-yl]amino}pyridin-3-yl)(piperazin-1-yl)methanone, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | 著者 | Shen, H.T, Xiao, Y.B, Yuan, K, Yang, P, Li, Q.N. | 登録日 | 2022-12-01 | 公開日 | 2023-12-13 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | Discovery of Potent DYRK2 Inhibitors with High Selectivity, Great Solubility, and Excellent Safety Properties for the Treatment of Prostate Cancer. J.Med.Chem., 66, 2023
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1IA8
| THE 1.7 A CRYSTAL STRUCTURE OF HUMAN CELL CYCLE CHECKPOINT KINASE CHK1 | 分子名称: | CHK1 CHECKPOINT KINASE, SULFATE ION | 著者 | Chen, P, Luo, C, Deng, Y, Ryan, K, Register, J, Margosiak, S, Tempczyk-Russell, A, Nguyen, B, Myers, P, Lundgren, K, Chen Kan, C.-C, O'Connor, P.M. | 登録日 | 2001-03-22 | 公開日 | 2001-04-18 | 最終更新日 | 2024-04-03 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | The 1.7 A crystal structure of human cell cycle checkpoint kinase Chk1: implications for Chk1 regulation. Cell(Cambridge,Mass.), 100, 2000
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6UNA
| Crystal structure of inactive p38gamma | 分子名称: | GLYCEROL, Mitogen-activated protein kinase 12, SULFATE ION | 著者 | Aoto, P.C, Stanfield, R.L, Wilson, I.A, Dyson, H.J, Wright, P.E. | 登録日 | 2019-10-11 | 公開日 | 2019-12-18 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.554 Å) | 主引用文献 | A Dynamic Switch in Inactive p38 gamma Leads to an Excited State on the Pathway to an Active Kinase. Biochemistry, 58, 2019
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6UIP
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6UNP
| Crystal structure of the kinase domain of BMPR2-D485G | 分子名称: | 1,2-ETHANEDIOL, ADENOSINE-5'-DIPHOSPHATE, Bone morphogenetic protein receptor type-2, ... | 著者 | Agnew, C, Jura, N. | 登録日 | 2019-10-13 | 公開日 | 2021-07-07 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | 主引用文献 | Structural basis for ALK2/BMPR2 receptor complex signaling through kinase domain oligomerization. Nat Commun, 12, 2021
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1J91
| Crystal structure of Z. mays CK2 kinase alpha subunit in complex with the ATP-competitive inhibitor 4,5,6,7-tetrabromobenzotriazole | 分子名称: | 4,5,6,7-TETRABROMOBENZOTRIAZOLE, CASEIN KINASE II, ALPHA CHAIN | 著者 | Battistutta, R, De Moliner, E, Sarno, S, Zanotti, G, Pinna, L.A. | 登録日 | 2001-05-23 | 公開日 | 2002-05-29 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | 主引用文献 | Structural features underlying selective inhibition of protein kinase CK2 by ATP site-directed tetrabromo-2-benzotriazole. Protein Sci., 10, 2001
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1J1B
| Binary complex structure of human tau protein kinase I with AMPPNP | 分子名称: | Glycogen synthase kinase-3 beta, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | 著者 | Aoki, M, Yokota, T, Sugiura, I, Sasaki, C, Hasegawa, T, Okumura, C, Kohno, T, Sugio, S, Matsuzaki, T. | 登録日 | 2002-12-03 | 公開日 | 2003-12-03 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Structural insight into nucleotide recognition in tau-protein kinase I/glycogen synthase kinase 3 beta. Acta Crystallogr.,Sect.D, 60, 2004
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1IG1
| 1.8A X-Ray structure of ternary complex of a catalytic domain of death-associated protein kinase with ATP analogue and Mn. | 分子名称: | MANGANESE (II) ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, death-associated protein kinase | 著者 | Tereshko, V, Teplova, M, Brunzelle, J, Watterson, D.M, Egli, M. | 登録日 | 2001-04-16 | 公開日 | 2002-04-01 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Crystal structures of the catalytic domain of human protein kinase associated with apoptosis and tumor suppression. Nat.Struct.Biol., 8, 2001
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1J3H
| Crystal structure of apoenzyme cAMP-dependent protein kinase catalytic subunit | 分子名称: | (4S)-2-METHYL-2,4-PENTANEDIOL, cAMP-dependent protein kinase, alpha-catalytic subunit | 著者 | Akamine, P, Madhusudan, Wu, J, Xuong, N.H, Ten Eyck, L.F, Taylor, S.S. | 登録日 | 2003-01-31 | 公開日 | 2003-03-04 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Dynamic Features of cAMP-dependent Protein Kinase Revealed by Apoenzyme Crystal Structure J.Mol.Biol., 327, 2003
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6UWY
| DYRK1A bound to a harmine derivative | 分子名称: | 4-(7-methoxy-1-methyl-9H-beta-carbolin-9-yl)butanamide, Dual specificity tyrosine-phosphorylation-regulated kinase 1A, TETRAETHYLENE GLYCOL | 著者 | Khamrui, S, Lazarus, M.B. | 登録日 | 2019-11-05 | 公開日 | 2020-02-12 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | 主引用文献 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human beta-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. J.Med.Chem., 63, 2020
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6V6A
| Inhibitory scaffolding of the ancient MAPK, ERK7 | 分子名称: | 1,2-ETHANEDIOL, Apical Cap Protein 9 (AC9), Mitogen-activated protein kinase | 著者 | Dewangan, P.S, O'Shaughnessy, W.J, Back, P.S, Hu, X, Bradley, P.J, Reese, M.L. | 登録日 | 2019-12-04 | 公開日 | 2020-05-27 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Ancient MAPK ERK7 is regulated by an unusual inhibitory scaffold required forToxoplasmaapical complex biogenesis. Proc.Natl.Acad.Sci.USA, 117, 2020
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1J1C
| Binary complex structure of human tau protein kinase I with ADP | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Glycogen synthase kinase-3 beta, MAGNESIUM ION | 著者 | Aoki, M, Yokota, T, Sugiura, I, Sasaki, C, Hasegawa, T, Okumura, C, Kohno, T, Sugio, S, Matsuzaki, T. | 登録日 | 2002-12-03 | 公開日 | 2003-12-03 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Structural insight into nucleotide recognition in tau-protein kinase I/glycogen synthase kinase 3 beta. Acta Crystallogr.,Sect.D, 60, 2004
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6V6L
| Co-structure of human glycogen synthase kinase beta with 1-(6-((2-((6-amino-5-nitropyridin-2-yl)amino)ethyl)amino)-2-(2,4-dichlorophenyl)pyridin-3-yl)-4-methylpiperazin-2-one | 分子名称: | 1-(6-((2-((6-amino-5-nitropyridin-2-yl)amino)ethyl)amino)-2-(2,4-dichlorophenyl)pyridin-3-yl)-4-methylpiperazin-2-one, Glycogen synthase kinase-3 beta, PHOSPHATE ION | 著者 | Bussiere, D.E, Fang, E, Shu, W. | 登録日 | 2019-12-05 | 公開日 | 2020-01-15 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | 主引用文献 | Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors. Bioorg.Med.Chem.Lett., 30, 2020
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1JAM
| Crystal structure of apo-form of Z. Mays CK2 protein kinase alpha subunit | 分子名称: | CASEIN KINASE II, ALPHA CHAIN | 著者 | Battistutta, R, De Moliner, E, Sarno, S, Zanotti, G, Pinna, L.A. | 登録日 | 2001-05-31 | 公開日 | 2002-05-31 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2.18 Å) | 主引用文献 | Structural features underlying selective inhibition of protein kinase CK2 by ATP site-directed tetrabromo-2-benzotriazole. Protein Sci., 10, 2001
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6VPG
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6VPM
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6VPI
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6VRE
| Structure of ASK1 bound to BIO-1772961 | 分子名称: | 3-methoxy-N-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-1-(pyrazin-2-yl)-1H-pyrazole-4-carboxamide, DIMETHYL SULFOXIDE, Mitogen-activated protein kinase kinase kinase 5 | 著者 | Chodaparambil, J.V, Marcotte, D.J. | 登録日 | 2020-02-07 | 公開日 | 2020-05-06 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.29 Å) | 主引用文献 | Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors. Acs Med.Chem.Lett., 11, 2020
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1JBP
| Crystal Structure of the Catalytic Subunit of cAMP-dependent Protein Kinase Complexed with a Substrate Peptide, ADP and Detergent | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, CAMP-DEPENDENT PROTEIN KINASE INHIBITOR, MUSCLE/BRAIN FORM, ... | 著者 | Madhusudan, Trafny, E.A, Xuong, N.H, Adams, J.A, Ten Eyck, L.F, Taylor, S.S, Sowadski, J.M. | 登録日 | 2001-06-06 | 公開日 | 2001-06-27 | 最終更新日 | 2023-08-16 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | cAMP-dependent protein kinase: crystallographic insights into substrate recognition and phosphotransfer. Protein Sci., 3, 1994
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6VPL
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6VRV
| Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model | 分子名称: | 4-chloro-1-{(1S)-1-[(3S)-3-fluoropyrrolidin-3-yl]ethyl}-3-methyl-1H-pyrrolo[2,3-b]pyridine-6-carboxamide, GLYCEROL, Serine/threonine-protein kinase pim-1 | 著者 | Barberis, C.E, Batchelor, J.D, Liu, J. | 登録日 | 2020-02-10 | 公開日 | 2020-11-04 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (1.74 Å) | 主引用文献 | Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model. Bioorg.Med.Chem.Lett., 30, 2020
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6VVG
| Structure of the Cydia pomonella Granulovirus kinase, PK-1 | 分子名称: | ADENOSINE MONOPHOSPHATE, Arginine kinase | 著者 | Oliver, M.R, Horne, C.R, Keown, J.R, Murphy, J.M, Metcalf, P. | 登録日 | 2020-02-17 | 公開日 | 2021-02-03 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | 主引用文献 | Granulovirus PK-1 kinase activity relies on a side-to-side dimerization mode centered on the regulatory alpha C helix. Nat Commun, 12, 2021
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