3EN6
 
 | | Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP102, a multitargeted kinase inhibitor | | 分子名称: | 1-(1-methylethyl)-3-quinolin-6-yl-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M. | | 登録日 | 2008-09-25 | | 公開日 | 2008-10-14 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.39 Å) | | 主引用文献 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
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3EN5
 | | Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP494, a multitargeted kinase inhibitor | | 分子名称: | 1-cyclobutyl-3-(3,4-dimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M. | | 登録日 | 2008-09-25 | | 公開日 | 2008-10-14 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.66 Å) | | 主引用文献 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
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3EN4
 | | Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP121, a multitargeted kinase inhibitor | | 分子名称: | 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M. | | 登録日 | 2008-09-25 | | 公開日 | 2008-10-14 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
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3EMG
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3EL8
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3EL7
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3EKN
 | | Insulin receptor kinase complexed with an inhibitor | | 分子名称: | 2-fluoro-6-{[2-({2-methoxy-4-[4-(1-methylethyl)piperazin-1-yl]phenyl}amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}benzamide, Insulin receptor | | 著者 | Chamberlain, S, Atkins, C, Deanda, F, Dumble, M, Gerding, R, Groy, A, Korenchuk, S, Kumar, R, Lei, H, Mook, R, Moorthy, G, Redman, A, Rowland, J, Shewchuk, L. | | 登録日 | 2008-09-19 | | 公開日 | 2008-12-30 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Bioorg.Med.Chem.Lett., 19, 2009
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3EKK
 | | Insulin receptor kinase complexed with an inhibitor | | 分子名称: | 2-[(2-{[1-(N,N-dimethylglycyl)-5-methoxy-1H-indol-6-yl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide, Insulin receptor | | 著者 | Chamberlain, S, Atkins, C, Deanda, F, Dumble, M, Gerding, R, Groy, A, Korenchuk, S, Kumar, R, Lei, H, Mook, R, Moorthy, G, Redman, A, Rowland, J, Sabbatini, P, Shewchuk, L. | | 登録日 | 2008-09-19 | | 公開日 | 2008-12-23 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase.
Bioorg.Med.Chem.Lett., 19, 2009
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3EFL
 | | Crystal structure of the VEGFR2 kinase domain in complex with motesanib | | 分子名称: | N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide, Vascular endothelial growth factor receptor 2 | | 著者 | Kim, J.L, Whittington, D.A, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | 登録日 | 2008-09-09 | | 公開日 | 2009-09-15 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery of Motesanib
To be Published
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3EFK
 | | Structure of c-Met with pyrimidone inhibitor 50 | | 分子名称: | 5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-2-[(4-fluorophenyl)amino]-3-methylpyrimidin-4(3H)-one, Hepatocyte growth factor receptor | | 著者 | Bellon, S.F, D'Angelo, N, Whittington, D, Dussault, I. | | 登録日 | 2008-09-09 | | 公開日 | 2008-10-07 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Design, synthesis, and biological evaluation of potent c-Met inhibitors.
J.Med.Chem., 51, 2008
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3EFJ
 | | Structure of c-Met with pyrimidone inhibitor 7 | | 分子名称: | 2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methylpyrimidin-4(3H)-one, Hepatocyte growth factor receptor | | 著者 | D'Angelo, N, Bellon, S, Whittington, D. | | 登録日 | 2008-09-09 | | 公開日 | 2008-10-07 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Design, synthesis, and biological evaluation of potent c-Met inhibitors.
J.Med.Chem., 51, 2008
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3E64
 | | Fragment based discovery of JAK-2 inhibitors | | 分子名称: | 4-(3-amino-1H-indazol-5-yl)-N-tert-butylbenzenesulfonamide, Tyrosine-protein kinase JAK2 | | 著者 | Antonysamy, S, Fang, W, Hirst, G, Park, F, Russell, M, Smyth, L, Sprengeler, P, Stappenbeck, F, Steensma, R, Thompson, D.A, Wilson, M, Wong, M, Zhang, A, Zhang, F. | | 登録日 | 2008-08-14 | | 公開日 | 2008-10-14 | | 最終更新日 | 2012-02-08 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Fragment-based discovery of JAK-2 inhibitors.
Bioorg.Med.Chem.Lett., 19, 2009
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3E63
 | | Fragment based discovery of JAK-2 inhibitors | | 分子名称: | 5-phenyl-1H-indazol-3-amine, Tyrosine-protein kinase JAK2 | | 著者 | Antonysamy, S, Fang, W, Hirst, G, Park, F, Russell, M, Smyth, L, Sprengeler, P, Stappenbeck, F, Steensma, R, Thompson, D.A, Wilson, M, Wong, M, Zhang, A, Zhang, F. | | 登録日 | 2008-08-14 | | 公開日 | 2008-10-14 | | 最終更新日 | 2012-02-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Fragment-based discovery of JAK-2 inhibitors.
Bioorg.Med.Chem.Lett., 19, 2009
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3E62
 | | Fragment based discovery of JAK-2 inhibitors | | 分子名称: | 5-bromo-1H-indazol-3-amine, Tyrosine-protein kinase JAK2 | | 著者 | Antonysamy, S, Fang, W, Hirst, G, Park, F, Russell, M, Smyth, L, Sprengeler, P, Stappenbeck, F, Steensma, R, Thompson, D.A, Wilson, M, Wong, M, Zhang, A, Zhang, F. | | 登録日 | 2008-08-14 | | 公開日 | 2008-10-14 | | 最終更新日 | 2012-02-08 | | 実験手法 | X-RAY DIFFRACTION (1.922 Å) | | 主引用文献 | Fragment-based discovery of JAK-2 inhibitors.
Bioorg.Med.Chem.Lett., 19, 2009
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3DZQ
 | | Human EphA3 kinase domain in complex with inhibitor AWL-II-38.3 | | 分子名称: | EPH receptor A3, N-[2-methyl-5-({[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]carbonyl}amino)phenyl]isoxazole-5-carboxamide | | 著者 | Walker, J.R, Syeda, F, Gray, N, Mansoor, W, Mackenzie, F, Bountra, C, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | 登録日 | 2008-07-30 | | 公開日 | 2008-08-26 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Kinase Domain of Human Ephrin Type-A Receptor 3 (Epha3) in Complex with ALW-II-38-3.
To be Published
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3DTW
 | | Crystal structure of the VEGFR2 kinase domain in complex with a benzisoxazole inhibitor | | 分子名称: | 6-chloro-N-pyrimidin-5-yl-3-{[3-(trifluoromethyl)phenyl]amino}-1,2-benzisoxazole-7-carboxamide, Vascular endothelial growth factor receptor 2 | | 著者 | Whittington, D.A, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | 登録日 | 2008-07-16 | | 公開日 | 2008-09-09 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Bioorg.Med.Chem.Lett., 18, 2008
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3DQX
 | | chicken c-Src kinase domain in complex with ATPgS | | 分子名称: | ADENOSINE MONOPHOSPHATE, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Azam, M, Seeliger, M.A, Gray, N, Kuriyan, J, Daley, G.Q. | | 登録日 | 2008-07-09 | | 公開日 | 2008-09-23 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Nat.Struct.Mol.Biol., 15, 2008
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3DQW
 | | c-Src kinase domain Thr338Ile mutant in complex with ATPgS | | 分子名称: | MAGNESIUM ION, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Azam, M, Seeliger, M.A, Gray, N, Kuriyan, J, Daley, G.Q. | | 登録日 | 2008-07-09 | | 公開日 | 2008-09-23 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.017 Å) | | 主引用文献 | Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Nat.Struct.Mol.Biol., 15, 2008
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3DPK
 | | cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor | | 分子名称: | 8-cyclohexyl-N-methoxy-5-oxo-2-{[4-(2-pyrrolidin-1-ylethyl)phenyl]amino}-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, Macrophage colony-stimulating factor 1 receptor, Fibroblast growth factor receptor 1, ... | | 著者 | Schubert, C. | | 登録日 | 2008-07-08 | | 公開日 | 2009-02-17 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors
J.Med.Chem., 52, 2009
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3DKO
 | | Complex between the kinase domain of human ephrin type-a receptor 7 (epha7) and inhibitor alw-ii-49-7 | | 分子名称: | 5-[(2-methyl-5-{[3-(trifluoromethyl)phenyl]carbamoyl}phenyl)amino]pyridine-3-carboxamide, Ephrin type-A receptor 7 | | 著者 | Walker, J.R, Syeda, F, Gray, N, Butler-Cole, C, Bountra, C, Wolkstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | 登録日 | 2008-06-25 | | 公開日 | 2008-08-19 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Kinase domain of human ephrin type-a receptor 7 (epha7) in complex with ALW-II-49-7
To be Published
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3DKG
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3DKF
 | | Structure of MET receptor tyrosine kinase in complex with inhibitor SGX-523 | | 分子名称: | 6-{[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}quinoline, CHLORIDE ION, Hepatocyte growth factor receptor | | 著者 | Hendle, J. | | 登録日 | 2008-06-24 | | 公開日 | 2009-07-07 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Mol.Cancer Ther., 8, 2009
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3DKC
 | | Structure of MET receptor tyrosine kinase in complex with ATP | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, Hepatocyte growth factor receptor, ... | | 著者 | Hendle, J. | | 登録日 | 2008-06-24 | | 公開日 | 2009-07-07 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.52 Å) | | 主引用文献 | SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Mol.Cancer Ther., 8, 2009
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3DK7
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3DK6
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