3LOK
 
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3LPB
 | | Crystal structure of Jak2 complexed with a potent 2,8-diaryl-quinoxaline inhibitor | | 分子名称: | N-methyl-4-[3-(3,4,5-trimethoxyphenyl)quinoxalin-5-yl]benzenesulfonamide, Tyrosine-protein kinase JAK2 | | 著者 | Tavares, G.A, Pissot-Soldermann, C, Gerspacher, M, Furet, P, Kroemer, M. | | 登録日 | 2010-02-05 | | 公開日 | 2010-04-28 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors
Bioorg.Med.Chem.Lett., 20, 2010
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3LCD
 | | Inhibitor Bound to A DFG-In structure of the Kinase Domain of CSF-1R | | 分子名称: | Macrophage colony-stimulating factor 1 receptor, N~3~-(2,6-dichlorobenzyl)-5-(4-{[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl}phenyl)pyrazine-2,3-diamine, SULFATE ION | | 著者 | Kamtekar, S, Day, J.E, Reitz, B.A, Mathis, K.J, Meyers, M.J. | | 登録日 | 2010-01-10 | | 公開日 | 2010-03-02 | | 最終更新日 | 2017-07-26 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode
Bioorg.Med.Chem.Lett., 20, 2010
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3LCK
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3LXN
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3LCS
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3LCO
 | | Inhibitor Bound to A DFG-Out structure of the Kinase Domain of CSF-1R | | 分子名称: | 3-({4-methoxy-5-[(4-methoxybenzyl)oxy]pyridin-2-yl}methoxy)-5-(1-methyl-1H-pyrazol-4-yl)pyrazin-2-amine, Macrophage colony-stimulating factor 1 receptor | | 著者 | Kamtekar, S, Day, J.E, Reitz, B.A, Mathis, K.J, Meyers, M.J. | | 登録日 | 2010-01-11 | | 公開日 | 2010-09-15 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Bioorg.Med.Chem.Lett., 20, 2010
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3LW0
 | | IGF-1RK in complex with ligand MSC1609119A-1 | | 分子名称: | 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide, GLYCEROL, Insulin-like growth factor 1 receptor | | 著者 | Graedler, U, Heinrich, T, Boettcher, H, Blaukat, A, Shutes, A, Askew, B. | | 登録日 | 2010-02-23 | | 公開日 | 2010-09-29 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Allosteric IGF-1R Inhibitors.
Acs Med.Chem.Lett., 1, 2010
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3LXP
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3LQ8
 | | Structure of the kinase domain of c-Met bound to XL880 (GSK1363089) | | 分子名称: | Hepatocyte growth factor receptor, N-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | | 著者 | Lougheed, J.C, Stout, T.J. | | 登録日 | 2010-02-08 | | 公開日 | 2010-05-19 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases.
Cancer Res., 69, 2009
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3LXK
 | | Structural and Thermodynamic Characterization of the TYK2 and JAK3 Kinase Domains in Complex with CP-690550 and CMP-6 | | 分子名称: | 3-{(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxopropanenitrile, Tyrosine-protein kinase JAK3 | | 著者 | Chrencik, J.E, Patny, A, Leung, I.K, Korniski, B, Emmons, T.L, Benson, T.E. | | 登録日 | 2010-02-25 | | 公開日 | 2010-06-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.
J.Mol.Biol., 400, 2010
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3LXL
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3LVP
 | | Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor | | 分子名称: | 3-(4-chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, Insulin-like growth factor 1 receptor, ... | | 著者 | Maignan, S, Marquette, J.P, Guilloteau, J.P. | | 登録日 | 2010-02-22 | | 公開日 | 2010-07-21 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Design of Potent IGF1-R Inhibitors Related to Bis-azaindoles
Chem.Biol.Drug Des., 76, 2010
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3MS9
 | | ABL kinase in complex with imatinib and a fragment (FRAG1) in the myristate pocket | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, Tyrosine-protein kinase ABL1, ... | | 著者 | Cowan-Jacob, S.W, Rummel, G, Fendrich, G. | | 登録日 | 2010-04-29 | | 公開日 | 2010-05-26 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay.
J.Am.Chem.Soc., 132, 2010
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3MJ2
 | | X-ray crystal structure of ITK complexed with inhibitor BMS-509744 | | 分子名称: | N-[5-({5-[(4-acetylpiperazin-1-yl)carbonyl]-4-methoxy-2-methylphenyl}sulfanyl)-1,3-thiazol-2-yl]-4-({[(1S)-1,2,2-trimethylpropyl]amino}methyl)benzamide, Tyrosine-protein kinase ITK/TSK | | 著者 | Kuglstatter, A, Villasenor, A.G. | | 登録日 | 2010-04-12 | | 公開日 | 2010-06-30 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation.
Chem.Biol.Drug Des., 76, 2010
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3JS2
 | | Crystal structure of minimal kinase domain of fibroblast growth factor receptor 1 in complex with 5-(2-thienyl)nicotinic acid | | 分子名称: | 5-(2-thienyl)nicotinic acid, Basic fibroblast growth factor receptor 1, PHOSPHATE ION | | 著者 | Bae, J.H, Ravindranathan, K.P, Mandiyan, V, Ekkati, A.R, Schlessinger, J, Jorgensen, W.L. | | 登録日 | 2009-09-09 | | 公開日 | 2010-02-23 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening
J.Med.Chem., 53, 2010
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3K5V
 | | Structure of Abl kinase in complex with imatinib and GNF-2 | | 分子名称: | 3-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)benzamide, 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, ... | | 著者 | Cowan-Jacob, S.W, Fendrich, G, Rummel, G, Strauss, A. | | 登録日 | 2009-10-08 | | 公開日 | 2010-01-19 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.74 Å) | | 主引用文献 | Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
Nature, 463, 2010
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3MJ1
 | | X-ray crystal structure of ITK complexed with inhibitor RO5191614 | | 分子名称: | 7-[(4-methylpiperazin-1-yl)methyl]-4-[(3-methyl-1H-pyrazol-5-yl)amino]-2-(tetrahydro-2H-pyran-4-yl)phthalazin-1(2H)-one, Tyrosine-protein kinase ITK/TSK | | 著者 | Kuglstatter, A, Villasenor, A.G. | | 登録日 | 2010-04-12 | | 公開日 | 2010-06-30 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.72 Å) | | 主引用文献 | Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation.
Chem.Biol.Drug Des., 76, 2010
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3MSS
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3LZB
 | | EGFR kinase domain complexed with an imidazo[2,1-b]thiazole inhibitor | | 分子名称: | Epidermal growth factor receptor, N-[3-(5-{2-[(4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl}imidazo[2,1-b][1,3]thiazol-6-yl)phenyl]-2-phenylacetamide | | 著者 | Swinger, K.K. | | 登録日 | 2010-03-01 | | 公開日 | 2011-03-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Bioorg.Med.Chem.Lett., 20, 2010
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3KMM
 | | Structure of human LCK kinase with a small molecule inhibitor | | 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, Proto-oncogene tyrosine-protein kinase LCK, SULFATE ION | | 著者 | Graves, B.J, Surgenor, A, Harris, W, Smith, I, Orchard, S, Flotow, H, Murray, E. | | 登録日 | 2009-11-10 | | 公開日 | 2010-12-08 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure of human LCK kinase with a small molecule inhibitor
To be Published
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3L8V
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3L9P
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3KXX
 | | Structure of the mutant Fibroblast Growth Factor receptor 1 | | 分子名称: | Basic fibroblast growth factor receptor 1 | | 著者 | Bae, J.H, Boggon, T.J, Tome, F, Mandiyan, V, Lax, I, Schlessinger, J. | | 登録日 | 2009-12-04 | | 公開日 | 2010-03-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells.
Proc.Natl.Acad.Sci.USA, 107, 2010
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3KRJ
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