3FXX
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![BU of 3fxx by Molmil](/molmil-images/mine/3fxx) | Human EphA3 Kinase and Juxtamembrane Region Bound to Substrate KQWDNYE[pTyr]IW | 分子名称: | Ephrin type-A receptor 3, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | 著者 | Davis, T, Walker, J.R, Mackenzie, F, Weigelt, J, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | 登録日 | 2009-01-21 | 公開日 | 2009-02-03 | 最終更新日 | 2023-11-22 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | Structural recognition of an optimized substrate for the ephrin family of receptor tyrosine kinases. Febs J., 276, 2009
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3FUP
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![BU of 3fup by Molmil](/molmil-images/mine/3fup) | Crystal structures of JAK1 and JAK2 inhibitor complexes | 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 JAK2 | 著者 | Williams, N.K, Bamert, R.S, Patel, O, Fantino, E, Rossjohn, J, Lucet, I.S. | 登録日 | 2009-01-14 | 公開日 | 2009-02-10 | 最終更新日 | 2023-11-22 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains. J.Mol.Biol., 387, 2009
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3FQS
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![BU of 3fqs by Molmil](/molmil-images/mine/3fqs) | Crystal structure of spleen tyrosine kinase 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 SYK | 著者 | Kuglstatter, A, Villasenor, A.G. | 登録日 | 2009-01-07 | 公開日 | 2009-03-10 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes. Chem.Biol.Drug Des., 73, 2009
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3FQH
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3FQE
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![BU of 3fqe by Molmil](/molmil-images/mine/3fqe) | |
3F82
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3F6X
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![BU of 3f6x by Molmil](/molmil-images/mine/3f6x) | c-Src kinase domain in complex with small molecule inhibitor | 分子名称: | Proto-oncogene tyrosine-protein kinase Src, [4-({4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]quinazolin-2-yl}amino)phenyl]acetonitrile | 著者 | Seeliger, M.A, Statsuk, A.V, Maly, D.J, Patrick, P.Z, Kuriyan, J, Shokat, K.M. | 登録日 | 2008-11-06 | 公開日 | 2008-12-09 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | Tuning a three-component reaction for trapping kinase substrate complexes. J.Am.Chem.Soc., 130, 2008
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3F66
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![BU of 3f66 by Molmil](/molmil-images/mine/3f66) | Human c-Met Kinase in complex with quinoxaline inhibitor | 分子名称: | 3-[3-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)quinoxalin-5-yl]phenol, GAMMA-BUTYROLACTONE, Hepatocyte growth factor receptor, ... | 著者 | Meier, C, Ceska, T. | 登録日 | 2008-11-05 | 公開日 | 2008-12-23 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | 主引用文献 | Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase. Bioorg.Med.Chem.Lett., 19, 2009
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3F5P
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![BU of 3f5p by Molmil](/molmil-images/mine/3f5p) | Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor | 分子名称: | 4-[[3-chloro-4-(1-methylimidazol-2-yl)sulfanyl-phenyl]amino]-7-[3-(2-hydroxyethyl-methyl-amino)propoxy]-6-methoxy-quinoline-3-carbonitrile, Insulin-like growth factor 1 receptor | 著者 | Xu, W, Miller, L.M, Mayer, S.C, Berger, D.M, Boschelli, D.H, Boschelli, F. | 登録日 | 2008-11-04 | 公開日 | 2008-12-30 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment Bioorg.Med.Chem.Lett., 19, 2009
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3F3W
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![BU of 3f3w by Molmil](/molmil-images/mine/3f3w) | Drug resistant cSrc kinase domain in complex with inhibitor RL45 (Type II) | 分子名称: | 1-{4-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea, Proto-oncogene tyrosine-protein kinase Src | 著者 | Grutter, C, Kluter, S, Getlik, M, Rauh, D. | 登録日 | 2008-10-31 | 公開日 | 2009-06-02 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.6 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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3F3V
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![BU of 3f3v by Molmil](/molmil-images/mine/3f3v) | Kinase domain of cSrc in complex with inhibitor RL45 (Type II) | 分子名称: | 1-{4-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea, Proto-oncogene tyrosine-protein kinase Src | 著者 | Grutter, C, Kluter, S, Getlik, M, Rauh, D. | 登録日 | 2008-10-31 | 公開日 | 2009-06-02 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.6 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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3F3U
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![BU of 3f3u by Molmil](/molmil-images/mine/3f3u) | Kinase domain of cSrc in complex with inhibitor RL37 (Type III) | 分子名称: | 1-[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]-3-phenylurea, Proto-oncogene tyrosine-protein kinase Src | 著者 | Gruetter, C, Klueter, S, Getlik, M, Rauh, D. | 登録日 | 2008-10-31 | 公開日 | 2009-03-03 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | A new screening assay for allosteric inhibitors of cSrc Nat.Chem.Biol., 5, 2009
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3F3T
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![BU of 3f3t by Molmil](/molmil-images/mine/3f3t) | Kinase domain of cSrc in complex with inhibitor RL38 (Type III) | 分子名称: | 1-[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]-3-naphthalen-1-ylurea, Proto-oncogene tyrosine-protein kinase Src | 著者 | Gruetter, C, Klueter, S, Getlik, M, Rauh, D. | 登録日 | 2008-10-31 | 公開日 | 2009-03-03 | 最終更新日 | 2023-11-01 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | A new screening assay for allosteric inhibitors of cSrc Nat.Chem.Biol., 5, 2009
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3EYH
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![BU of 3eyh by Molmil](/molmil-images/mine/3eyh) | Crystal structures of JAK1 and JAK2 inhibitor complexes | 分子名称: | 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Tyrosine-protein kinase | 著者 | Williams, N.K, Bamert, R.S, Patell, O, Wang, C, Walden, P.M, Fantino, E. | 登録日 | 2008-10-20 | 公開日 | 2009-02-03 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains. J.Mol.Biol., 387, 2009
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3EYG
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![BU of 3eyg by Molmil](/molmil-images/mine/3eyg) | Crystal structures of JAK1 and JAK2 inhibitor complexes | 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 | 著者 | Williams, N.K, Bamert, R.S, Patell, O, Wang, C, Walden, P.M, Fantino, E. | 登録日 | 2008-10-20 | 公開日 | 2009-02-03 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains. J.Mol.Biol., 387, 2009
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3EWH
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![BU of 3ewh by Molmil](/molmil-images/mine/3ewh) | Crystal structure of the VEGFR2 kinase domain in complex with a pyridyl-pyrimidine benzimidazole inhibitor | 分子名称: | 1,2-ETHANEDIOL, N-[4-({3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl}oxy)naphthalen-1-yl]-6-(trifluoromethyl)-1H-benzimidazol-2-amine, vascular endothelial growth factor receptor 2 | 著者 | Whittington, D.A, Long, A.M, Rose, P, Gu, Y, Zhao, H. | 登録日 | 2008-10-15 | 公開日 | 2009-08-25 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | 主引用文献 | Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase. Bioorg.Med.Chem.Lett., 19, 2009
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3ETA
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![BU of 3eta by Molmil](/molmil-images/mine/3eta) | Kinase domain of insulin receptor complexed with a pyrrolo pyridine inhibitor | 分子名称: | 1-(3-{5-[4-(aminomethyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}phenyl)-3-(2-phenoxyphenyl)urea, insulin receptor, kinase domain | 著者 | Patnaik, S, Stevens, K, Gerding, R, Deanda, F, Shotwell, B, Tang, J, Hamajima, T, Nakamura, H, Leesnitzer, A, Hassell, A, Shewchuk, L, Kumar, R, Lei, H, Chamberlain, S. | 登録日 | 2008-10-07 | 公開日 | 2009-05-26 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. Bioorg.Med.Chem.Lett., 19, 2009
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3ET7
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![BU of 3et7 by Molmil](/molmil-images/mine/3et7) | Crystal structure of PYK2 complexed with PF-2318841 | 分子名称: | 5-{[4-{[2-(pyrrolidin-1-ylsulfonyl)benzyl]amino}-5-(trifluoromethyl)pyrimidin-2-yl]amino}-1,3-dihydro-2H-indol-2-one, PHOSPHATE ION, Protein tyrosine kinase 2 beta | 著者 | Han, S. | 登録日 | 2008-10-07 | 公開日 | 2009-06-23 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation. Bioorg.Med.Chem.Lett., 18, 2008
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3EQR
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![BU of 3eqr by Molmil](/molmil-images/mine/3eqr) | Crystal Structure of Ack1 with compound T74 | 分子名称: | Activated CDC42 kinase 1, CHLORIDE ION, N~3~-(2,6-dimethylphenyl)-1-(3-methoxy-3-methylbutyl)-N~6~-(4-piperazin-1-ylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine | 著者 | Liu, J, Wang, Z, Walker, N.P.C. | 登録日 | 2008-10-01 | 公開日 | 2008-12-02 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors. Bioorg.Med.Chem.Lett., 18, 2008
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3EQP
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![BU of 3eqp by Molmil](/molmil-images/mine/3eqp) | Crystal Structure of Ack1 with compound T95 | 分子名称: | Activated CDC42 kinase 1, CHLORIDE ION, N-(2,6-dimethylphenyl)-4-(2-ethoxyphenoxy)-2-({4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl}amino)pyrimidine-5-carboxamide | 著者 | Liu, J, Wang, Z, Walker, N.P.C. | 登録日 | 2008-10-01 | 公開日 | 2008-12-02 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | 主引用文献 | Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors. Bioorg.Med.Chem.Lett., 18, 2008
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3EN7
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![BU of 3en7 by Molmil](/molmil-images/mine/3en7) | Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with S1, a multitargeted kinase inhibitor | 分子名称: | 3-[4-AMINO-1-(1-METHYLETHYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL]PHENOL, 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 (2.81 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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3EN6
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![BU of 3en6 by Molmil](/molmil-images/mine/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
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![BU of 3en5 by Molmil](/molmil-images/mine/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
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![BU of 3en4 by Molmil](/molmil-images/mine/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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![BU of 3emg by Molmil](/molmil-images/mine/3emg) | |