3PRF
 
 | | Crystal Structure of Human B-Raf Kinase Domain in Complex with a Non-Oxime Furopyridine Inhibitor | | 分子名称: | 2-chloro-5-{[2-(pyrimidin-2-yl)furo[2,3-c]pyridin-3-yl]amino}phenol, Serine/threonine-protein kinase B-raf | | 著者 | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | 登録日 | 2010-11-29 | | 公開日 | 2011-02-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PPZ
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3PPK
 | | Human B-Raf Kinase in Complex with a Non-Oxime Furopyridine Inhibitor | | 分子名称: | 3-[(5-hydroxynaphthalen-2-yl)amino]-N-(pyrimidin-4-yl)furo[2,3-c]pyridine-2-carboxamide, Serine/threonine-protein kinase B-raf | | 著者 | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | 登録日 | 2010-11-24 | | 公開日 | 2011-02-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PPJ
 | | Human B-Raf Kinase in Complex with a Furopyridine Inhibitor | | 分子名称: | Serine/threonine-protein kinase B-raf, methyl 3-{[(5S)-1-(hydroxyamino)-5H-inden-5-yl]amino}furo[2,3-c]pyridine-2-carboxylate | | 著者 | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | 登録日 | 2010-11-24 | | 公開日 | 2011-02-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.7 Å) | | 主引用文献 | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PP0
 | | Crystal Structure of the Kinase domain of Human HER2 (erbB2). | | 分子名称: | 2-{2-[4-({5-chloro-6-[3-(trifluoromethyl)phenoxy]pyridin-3-yl}amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethoxy}ethanol, Receptor tyrosine-protein kinase erbB-2 | | 著者 | Skene, R.J, Aertgeerts, K, Sogabe, S. | | 登録日 | 2010-11-23 | | 公開日 | 2011-03-30 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein.
J.Biol.Chem., 286, 2011
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3POZ
 | | EGFR Kinase domain complexed with tak-285 | | 分子名称: | Epidermal growth factor receptor, N-{2-[4-({3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl}amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl}-3-hydroxy-3-methylbutanamide, SULFATE ION | | 著者 | Aertgeerts, K, Skene, R, Sogabe, S. | | 登録日 | 2010-11-23 | | 公開日 | 2011-03-30 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein.
J.Biol.Chem., 286, 2011
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3PLS
 | | RON in complex with ligand AMP-PNP | | 分子名称: | MAGNESIUM ION, Macrophage-stimulating protein receptor, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | 著者 | Wang, J, Steinbacher, S, Augustin, M, Schreiner, P, Epstein, D, Mulvihill, M.J, Crew, A.P. | | 登録日 | 2010-11-15 | | 公開日 | 2010-11-24 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.24 Å) | | 主引用文献 | The Crystal Structure of a Constitutively Active Mutant RON Kinase Suggests an Intramolecular Autophosphorylation Hypothesis
Biochemistry, 49, 2010
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3PJC
 | | Crystal structure of JAK3 complexed with a potent ATP site inhibitor showing high selectivity within the Janus kinase family | | 分子名称: | 3-(1H-indol-3-yl)-4-[2-(4-oxopiperidin-1-yl)-5-(trifluoromethyl)pyrimidin-4-yl]-1H-pyrrole-2,5-dione, Tyrosine-protein kinase JAK3 | | 著者 | Tavares, G.A, Thoma, G, Zerwes, H.-G, Kroemer, M. | | 登録日 | 2010-11-09 | | 公開日 | 2010-12-29 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family.
J.Med.Chem., 54, 2011
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3PJ3
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3PJ2
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3PJ1
 | | Crystal structure of BTK kinase domain complexed with 3-(2,6-Dichloro-phenyl)-7-[4-(2-diethylamino-ethoxy)-phenylamino]-1-methyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one | | 分子名称: | 3-(2,6-dichlorophenyl)-7-({4-[2-(diethylamino)ethoxy]phenyl}amino)-1-methyl-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, Tyrosine-protein kinase BTK | | 著者 | Kuglstatter, A, Wong, A. | | 登録日 | 2010-11-08 | | 公開日 | 2011-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures.
Protein Sci., 20, 2011
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3PIZ
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3PIY
 | | Crystal structure of BTK kinase domain complexed with R406 | | 分子名称: | 6-({5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]pyrimidin-4-yl}amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one, Tyrosine-protein kinase BTK | | 著者 | Kuglstatter, A, Wong, A. | | 登録日 | 2010-11-08 | | 公開日 | 2011-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures.
Protein Sci., 20, 2011
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3PIX
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3P86
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3P08
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3OY3
 | | Crystal structure of ABL T315I mutant kinase domain bound with a DFG-out inhibitor AP24589 | | 分子名称: | 5-[(5-{[4-{[4-(2-hydroxyethyl)piperazin-1-yl]methyl}-3-(trifluoromethyl)phenyl]carbamoyl}-2-methylphenyl)ethynyl]-1-methyl-1H-imidazole-2-carboxamide, Tyrosine-protein kinase ABL1 | | 著者 | Zhou, T, Commodore, L, Huang, W.S, Wang, Y, Thomas, M, Keats, J, Xu, Q, Rivera, V, Shakespeare, W.C, Clackson, T, Dalgarno, D.C, Zhu, X. | | 登録日 | 2010-09-22 | | 公開日 | 2010-12-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance.
Chem.Biol.Drug Des., 77, 2011
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3OXZ
 | | Crystal structure of ABL kinase domain bound with a DFG-out inhibitor AP24534 | | 分子名称: | 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide, Tyrosine-protein kinase ABL1 | | 著者 | Zhou, T, Huang, W.S, Wang, Y, Thomas, M, Keats, J, Xu, Q, Rivera, V, Shakespeare, W.C, Clackson, T, Dalgarno, D.C, Zhu, X. | | 登録日 | 2010-09-22 | | 公開日 | 2010-12-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance.
Chem.Biol.Drug Des., 77, 2011
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3OG7
 | | B-Raf Kinase V600E oncogenic mutant in complex with PLX4032 | | 分子名称: | AKAP9-BRAF fusion protein, N-(3-{[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonamide | | 著者 | Zhang, Y, Zhang, K.Y, Zhang, C. | | 登録日 | 2010-08-16 | | 公開日 | 2010-09-22 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | | 主引用文献 | Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.
Nature, 467, 2010
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3OF0
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3OEZ
 | | crystal structure of the L317I mutant of the chicken c-Src tyrosine kinase domain complexed with imatinib | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, ACETATE ION, GLYCEROL, ... | | 著者 | Boubeva, R, Pernot, L, Perozzo, R, Scapozza, L. | | 登録日 | 2010-08-13 | | 公開日 | 2011-08-17 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | a single amino-acid dictates the dynamics of the switch between active and inactive C-Src conformation
To be Published
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3OCT
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3OCS
 | | Crystal structure of bruton's tyrosine kinase in complex with inhibitor CGI1746 | | 分子名称: | 4-tert-butyl-N-[2-methyl-3-(4-methyl-6-{[4-(morpholin-4-ylcarbonyl)phenyl]amino}-5-oxo-4,5-dihydropyrazin-2-yl)phenyl]benzamide, BETA-MERCAPTOETHANOL, SULFATE ION, ... | | 著者 | Davies, D.R, Gallion, S.L, Staker, B.L. | | 登録日 | 2010-08-10 | | 公開日 | 2010-11-03 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | A novel, specific Btk inhibitor antagonizes BCR and Fc[gamma]R signaling and suppresses inflammatory arthritis
To be Published
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3O23
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3NZ0
 | | Non-phosphorylated TYK2 kinase with CMP6 | | 分子名称: | 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Non-receptor tyrosine-protein kinase TYK2 | | 著者 | Eigenbrot, C, Ultsch, M. | | 登録日 | 2010-07-15 | | 公開日 | 2010-10-20 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | A new regulatory switch in a JAK protein kinase.
Proteins, 79, 2011
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