3IO7
 
 | | 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2 | | 分子名称: | (3S)-1-[6-(2-aminopyrazolo[1,5-a]pyrimidin-3-yl)pyrimidin-4-yl]-N,N-diethylpiperidine-3-carboxamide, Tyrosine-protein kinase JAK2 | | 著者 | Zuccola, H.J, Ledeboer, M.W, Pierce, A.C. | | 登録日 | 2009-08-13 | | 公開日 | 2009-11-10 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Bioorg.Med.Chem.Lett., 19, 2009
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3IKA
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3IK3
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3II5
 | | The Complex of wild-type B-RAF with Pyrazolo pyrimidine inhibitor | | 分子名称: | B-Raf proto-oncogene serine/threonine-protein kinase, N-[3-(3-{4-[(dimethylamino)methyl]phenyl}pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-3-(trifluoromethyl)benzamide, PHOSPHATE ION | | 著者 | Xu, W, Breger, D, Torres, N, Dutia, M, Powell, D, Ciszewski, G. | | 登録日 | 2009-07-31 | | 公開日 | 2009-11-10 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.79 Å) | | 主引用文献 | Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Bioorg.Med.Chem.Lett., 19, 2009
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3IDP
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3I81
 | | Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with BMS-754807 [1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoro-3-pyridinyl)-2-methyl-L-prolinamide] | | 分子名称: | 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-proli namide, Insulin-like growth factor 1 receptor | | 著者 | Sack, J.S. | | 登録日 | 2009-07-09 | | 公開日 | 2009-12-22 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.08 Å) | | 主引用文献 | Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
J.Med.Chem., 52, 2009
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3I5N
 | | Crystal structure of c-Met with triazolopyridazine inhibitor 13 | | 分子名称: | 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine, Hepatocyte growth factor receptor | | 著者 | Bellon, S.F, Whittington, D.A, Long, A.M, Boezio, A.A. | | 登録日 | 2009-07-06 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors
Bioorg.Med.Chem.Lett., 19, 2009
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3HNG
 | | Crystal structure of VEGFR1 in complex with N-(4-Chlorophenyl)-2-((pyridin-4-ylmethyl)amino)benzamide | | 分子名称: | CHLORIDE ION, N-(4-chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide, Vascular endothelial growth factor receptor 1 | | 著者 | Tresaugues, L, Roos, A, Arrowsmith, C.H, Berglund, H, Bountra, C, Collins, R, Edwards, A.M, Flodin, S, Flores, A, Graslund, S, Hammarstrom, M, Johansson, A, Johansson, I, Karlberg, T, Kotenyova, T, Moche, M, Nyman, T, Persson, C, Kragh-Nielsen, T, Kotzch, A, Sagemark, J, Schueler, H, Schutz, P, Siponen, M.I, Svensson, L, Thorsell, A.G, Van der Berg, S, Weigelt, J, Welin, M, Wisniewska, M, Nordlund, P, Structural Genomics Consortium (SGC) | | 登録日 | 2009-05-31 | | 公開日 | 2009-06-30 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Crystal structure of VEGFR1 in complex with N-(4-Chlorophenyl)-2-((pyridin-4-ylmethyl)amino)benzamide
To be Published
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3HMI
 | | The crystal structure of human ABL2 in complex with 5-AMINO-3-{[4-(AMINOSULFONYL)PHENYL]AMINO}-N-(2,6-DIFLUOROPHENYL)-1H-1,2,4-TRIAZOLE-1-CARBOTHIOAMIDE | | 分子名称: | 5-AMINO-3-{[4-(AMINOSULFONYL)PHENYL]AMINO}-N-(2,6-DIFLUOROPHENYL)-1H-1,2,4-TRIAZOLE-1-CARBOTHIOAMIDE, Tyrosine-protein kinase ABL2 | | 著者 | Ugochukwu, E, Salah, E, Barr, A, Mahajan, P, Shrestha, B, Savitsky, P, Chaikuad, A, Allerston, C, von Delft, F, Bountra, C, Arrowsmith, C.H, Weigelt, J, Edwards, A, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2009-05-29 | | 公開日 | 2009-07-07 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | The crystal structure of human ABL2 in complex with 5-AMINO-3-{[4-(AMINOSULFONYL)PHENYL]AMINO}-N-(2,6-DIFLUOROPHENYL)-1H-1,2,4-TRIAZOLE-1-CARBOTHIOAMIDE
To be Published
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3HGK
 | | crystal structure of effect protein AvrptoB complexed with kinase Pto | | 分子名称: | Effector protein hopAB2, Protein kinase | | 著者 | Dong, J, Fan, F, Gu, L, Chai, J. | | 登録日 | 2009-05-14 | | 公開日 | 2009-06-23 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Crystal Structure of the Complex between Pseudomonas Effector AvrPtoB and the Tomato Pto Kinase Reveals Both a Shared and a Unique Interface Compared with AvrPto-Pto
Plant Cell, 21, 2009
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3H3C
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3GVU
 | | The crystal structure of human ABL2 in complex with GLEEVEC | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Tyrosine-protein kinase ABL2 | | 著者 | Ugochukwu, E, Salah, E, Barr, A, Mahajan, P, Shrestha, B, Savitsky, P, Chaikuad, A, Filippakopoulos, P, Roos, A, Pike, A.C.W, von Delft, F, Bountra, C, Arrowsmith, C.H, Weigelt, J, Edwards, A, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2009-03-31 | | 公開日 | 2009-04-21 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | The crystal structure of human ABL2 in complex with GLEEVEC
To be Published
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3GT8
 | | Crystal structure of the inactive EGFR kinase domain in complex with AMP-PNP | | 分子名称: | Epidermal growth factor receptor, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Jura, N, Endres, N.F, Engel, K, Deindl, S, Das, R, Lamers, M.H, Wemmer, D.E, Zhang, X, Kuriyan, J. | | 登録日 | 2009-03-27 | | 公開日 | 2009-07-21 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.955 Å) | | 主引用文献 | Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segment.
Cell(Cambridge,Mass.), 137, 2009
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3GQL
 | | Crystal Structure of activated receptor tyrosine kinase in complex with substrates | | 分子名称: | (E)-[4-(3,5-difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol, Basic fibroblast growth factor receptor 1 | | 著者 | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | | 登録日 | 2009-03-24 | | 公開日 | 2009-08-18 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.
Cell(Cambridge,Mass.), 138, 2009
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3GQI
 | | Crystal Structure of activated receptor tyrosine kinase in complex with substrates | | 分子名称: | Basic fibroblast growth factor receptor 1, DECAVANADATE, MAGNESIUM ION, ... | | 著者 | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | | 登録日 | 2009-03-24 | | 公開日 | 2009-08-18 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.
Cell(Cambridge,Mass.), 138, 2009
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3GOP
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3GEQ
 | | Structural basis for the chemical rescue of Src kinase activity | | 分子名称: | 1-TERT-BUTYL-3-(4-CHLORO-PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Muratore, K.E, Seeliger, M.A, Wang, Z, Fomina, D, Neiswinger, J, Havranek, J.J, Baker, D, Kuriyan, J, Cole, P.A. | | 登録日 | 2009-02-25 | | 公開日 | 2009-04-28 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Comparative analysis of mutant tyrosine kinase chemical rescue.
Biochemistry, 48, 2009
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3GEN
 | | The 1.6 A crystal structure of human bruton's tyrosine kinase bound to a pyrrolopyrimidine-containing compound | | 分子名称: | 4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl-cyclopentane, Tyrosine-protein kinase BTK | | 著者 | Marcotte, D.J, Liu, Y.T, Arduini, R.M, Hession, C.A, Miatkowski, K, Wildes, C.P, Cullen, P.F, Hopkins, B, Mertsching, E, Jenkins, T.J, Romanowski, M.J, Baker, D.P, Silvian, L.F. | | 登録日 | 2009-02-25 | | 公開日 | 2010-01-19 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases.
Protein Sci., 19, 2010
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3G6H
 | | Src Thr338Ile inhibited in the DFG-Asp-Out conformation | | 分子名称: | N-{4-methyl-3-[(3-{4-[(3,4,5-trimethoxyphenyl)amino]-1,3,5-triazin-2-yl}pyridin-2-yl)amino]phenyl}-3-(trifluoromethyl)benzamide, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Seeliger, M.A, Ranjitkar, P, Kasap, C, Shan, Y, Shaw, D.E, Shah, N.P, Kuriyan, J, Maly, D.J. | | 登録日 | 2009-02-06 | | 公開日 | 2009-03-24 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | | 主引用文献 | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
Cancer Res., 69, 2009
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3G6G
 | | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations | | 分子名称: | GLYCEROL, N-{3-[(3-{4-[(4-methoxyphenyl)amino]-1,3,5-triazin-2-yl}pyridin-2-yl)amino]-4-methylphenyl}-4-[(4-methylpiperazin-1-yl)methyl]benzamide, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Seeliger, M.A, Ranjitkar, P, Kasap, C, Shan, Y, Shaw, D.E, Shah, N.P, Kuriyan, J, Maly, D.J. | | 登録日 | 2009-02-06 | | 公開日 | 2009-03-24 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.31 Å) | | 主引用文献 | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
Cancer Res., 69, 2009
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3G5D
 | | Kinase domain of cSrc in complex with Dasatinib | | 分子名称: | GLYCEROL, N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Grutter, C, Kluter, S, Rauh, D. | | 登録日 | 2009-02-05 | | 公開日 | 2009-06-02 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc
J.Med.Chem., 52, 2009
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3G0F
 | | KIT kinase domain mutant D816H in complex with sunitinib | | 分子名称: | Mast/stem cell growth factor receptor, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo xamide, SULFATE ION | | 著者 | Gajiwala, K.S, Wu, J.C, Lunney, E.A, Demetri, G.D. | | 登録日 | 2009-01-27 | | 公開日 | 2009-02-24 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3G0E
 | | KIT kinase domain in complex with sunitinib | | 分子名称: | Mast/stem cell growth factor receptor, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo xamide | | 著者 | Gajiwala, K.S, Wu, J.C, Lunney, E.A, Gemetri, G.D. | | 登録日 | 2009-01-27 | | 公開日 | 2009-02-24 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3FZT
 | | Crystal structure of PYK2 complexed with PF-4618433 | | 分子名称: | 1-[5-tert-butyl-2-(4-methylphenyl)-1,2-dihydro-3H-pyrazol-3-ylidene]-3-{3-[(pyridin-3-yloxy)methyl]-1H-pyrazol-5-yl}urea, Protein tyrosine kinase 2 beta | | 著者 | Han, S. | | 登録日 | 2009-01-26 | | 公開日 | 2009-03-31 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.
J.Biol.Chem., 284, 2009
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3FZS
 | | Crystal Structure of PYK2 complexed with BIRB796 | | 分子名称: | 1-(5-TERT-BUTYL-2-P-TOLYL-2H-PYRAZOL-3-YL)-3-[4-(2-MORPHOLIN-4-YL-ETHOXY)-NAPHTHALEN-1-YL]-UREA, Protein tyrosine kinase 2 beta | | 著者 | Han, S. | | 登録日 | 2009-01-26 | | 公開日 | 2009-03-31 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.
J.Biol.Chem., 284, 2009
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