5WO4
 
 | | JAK1 complexed with compound 28 | | 分子名称: | 3-[(4-chloro-3-methoxyphenyl)amino]-1-[(3R,4S)-4-cyanooxan-3-yl]-1H-pyrazole-4-carboxamide, Tyrosine-protein kinase JAK1 | | 著者 | Lesburg, C.A, Patel, S.B. | | 登録日 | 2017-08-01 | | 公開日 | 2017-12-06 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.84 Å) | | 主引用文献 | The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
J. Med. Chem., 60, 2017
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5WIN
 | | JAK2 Pseudokinase in complex with JNJ7706621 | | 分子名称: | 4-({5-amino-1-[(2,6-difluorophenyl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)benzenesulfonamide, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.38 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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2P2H
 | | Crystal structure of the VEGFR2 kinase domain in complex with a pyridinyl-triazine inhibitor | | 分子名称: | 4-(2-anilinopyridin-3-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine, Vascular endothelial growth factor receptor 2 | | 著者 | Whittington, D.A, Kim, J.L, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | 登録日 | 2007-03-07 | | 公開日 | 2007-03-20 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor
J.Med.Chem., 50, 2007
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5W86
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2P4I
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2P2I
 | | Crystal structure of the VEGFR2 kinase domain in complex with a nicotinamide inhibitor | | 分子名称: | N-(4-phenoxyphenyl)-2-[(pyridin-4-ylmethyl)amino]nicotinamide, Vascular endothelial growth factor receptor 2 | | 著者 | Whittington, D.A, Kim, J.L, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | 登録日 | 2007-03-07 | | 公開日 | 2007-03-20 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor
J.Med.Chem., 50, 2007
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2P0C
 | | Catalytic Domain of the Proto-oncogene Tyrosine-protein Kinase MER | | 分子名称: | BETA-MERCAPTOETHANOL, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Walker, J.R, Huang, X, Finerty Jr, P.J, Weigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | 登録日 | 2007-02-28 | | 公開日 | 2007-05-08 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural insights into the inhibited states of the Mer receptor tyrosine kinase.
J.Struct.Biol., 165, 2009
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2OSC
 | | Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors | | 分子名称: | Angiopoietin-1 receptor, N-{4-METHYL-3-[(3-PYRIMIDIN-4-YLPYRIDIN-2-YL)AMINO]PHENYL}-3-(TRIFLUOROMETHYL)BENZAMIDE | | 著者 | Bellon, S.F, Kim, J. | | 登録日 | 2007-02-05 | | 公開日 | 2007-03-20 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Bioorg.Med.Chem.Lett., 17, 2007
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5VND
 | | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide, ... | | 著者 | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | | 登録日 | 2017-04-30 | | 公開日 | 2017-05-24 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Cancer Res., 77, 2017
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5WEV
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5WFJ
 | | THE JAK3 KINASE DOMAIN IN COMPLEX WITH A COVALENT INHIBITOR | | 分子名称: | 4-({[3-(propanoylamino)phenyl]methyl}amino)pyrrolo[1,2-b]pyridazine-3-carboxamide, Tyrosine-protein kinase JAK3 | | 著者 | Sack, J. | | 登録日 | 2017-07-12 | | 公開日 | 2017-10-04 | | 最終更新日 | 2017-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.48 Å) | | 主引用文献 | Discovery of highly potent, selective, covalent inhibitors of JAK3.
Bioorg. Med. Chem. Lett., 27, 2017
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2OIC
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2OJ9
 | | Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor | | 分子名称: | 3-[5-(1H-IMIDAZOL-1-YL)-7-METHYL-1H-BENZIMIDAZOL-2-YL]-4-[(PYRIDIN-2-YLMETHYL)AMINO]PYRIDIN-2(1H)-ONE, Insulin-like growth factor 1 receptor precursor (EC 2.7.10.1) (Insulin-like growth factor I receptor) (IGF-I receptor) (CD221 antigen) | | 著者 | Sack, J.S, Jacobson, B.L. | | 登録日 | 2007-01-12 | | 公開日 | 2007-05-01 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).
Bioorg.Med.Chem.Lett., 17, 2007
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2OG8
 | | crystal structure of aminoquinazoline 36 bound to Lck | | 分子名称: | N-{2-[(N,N-DIETHYLGLYCYL)AMINO]-5-(TRIFLUOROMETHYL)PHENYL}-4-METHYL-3-[2-(METHYLAMINO)QUINAZOLIN-6-YL]BENZAMIDE, Proto-oncogene tyrosine-protein kinase LCK | | 著者 | Huang, X. | | 登録日 | 2007-01-05 | | 公開日 | 2007-02-27 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck: Synthesis, SAR, and in Vivo Anti-Inflammatory Activity
J.Med.Chem., 49, 2006
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5XDL
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2PWL
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2PVF
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2OF2
 | | crystal structure of furanopyrimidine 8 bound to lck | | 分子名称: | 2,3-DIPHENYL-N-(2-PIPERAZIN-1-YLETHYL)FURO[2,3-B]PYRIDIN-4-AMINE, Proto-oncogene tyrosine-protein kinase LCK | | 著者 | Martin, M.W. | | 登録日 | 2007-01-02 | | 公開日 | 2007-02-27 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: Synthesis, SAR, and pharmacokinetic properties.
Bioorg.Med.Chem.Lett., 17, 2007
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5XP7
 | | C-Src in complex with ATP-CHCl | | 分子名称: | GLYCEROL, MAGNESIUM ION, Proto-oncogene tyrosine-protein kinase Src, ... | | 著者 | Guo, M, Dai, S, Duan, Y, Chen, L, Chen, Y. | | 登録日 | 2017-06-01 | | 公開日 | 2017-09-06 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.012 Å) | | 主引用文献 | Remarkably Stereospecific Utilization of ATP alpha , beta-Halomethylene Analogues by Protein Kinases.
J. Am. Chem. Soc., 139, 2017
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2OID
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2OO8
 | | Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors | | 分子名称: | Angiopoietin-1 receptor, N-{3-[3-(DIMETHYLAMINO)PROPYL]-5-(TRIFLUOROMETHYL)PHENYL}-4-METHYL-3-[(3-PYRIMIDIN-4-YLPYRIDIN-2-YL)AMINO]BENZAMIDE | | 著者 | Bellon, S.F, Kim, J. | | 登録日 | 2007-01-25 | | 公開日 | 2007-03-20 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Bioorg.Med.Chem.Lett., 17, 2007
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2PL0
 | | LCK bound to imatinib | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Proto-oncogene tyrosine-protein kinase LCK | | 著者 | Jacobs, M.D. | | 登録日 | 2007-04-18 | | 公開日 | 2007-10-09 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Classifying protein kinase structures guides use of ligand-selectivity profiles to predict inactive conformations: Structure of lck/imatinib complex.
Proteins, 70, 2007
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2OIQ
 | | Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib. | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, GLYCEROL, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Seeliger, M.A, Nagar, B, Frank, F, Cao, X, Henderson, M.N, Kuriyan, J. | | 登録日 | 2007-01-11 | | 公開日 | 2007-03-20 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.07 Å) | | 主引用文献 | c-Src Binds to the Cancer Drug Imatinib with an Inactive Abl/c-Kit Conformation and a Distributed Thermodynamic Penalty.
Structure, 15, 2007
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2OGV
 | | Crystal Structure of the Autoinhibited Human c-Fms Kinase Domain | | 分子名称: | Macrophage colony-stimulating factor 1 receptor precursor | | 著者 | Walter, M, Lucet, I.S, Patel, O, Broughton, S.E, Bamert, R, Williams, N.K, Fantino, E, Wilks, A.F, Rossjohn, J. | | 登録日 | 2007-01-09 | | 公開日 | 2007-02-06 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | The 2.7 A crystal structure of the autoinhibited human c-Fms kinase domain.
J.Mol.Biol., 367, 2007
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5X2A
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