4RJ4
 
 | | EGFR kinase (T790M/L858R) with inhibitor compound 6 | | 分子名称: | Epidermal growth factor receptor, N-[2-(4-methoxypiperidin-1-yl)pyrimidin-4-yl]-1-(propan-2-yl)-2-(1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridin-6-amine | | 著者 | Eigenbrot, C, Yu, C. | | 登録日 | 2014-10-08 | | 公開日 | 2014-11-26 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.78 Å) | | 主引用文献 | Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation.
J.Med.Chem., 57, 2014
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4RIY
 | | Crystal structure of an EGFR/HER3 kinase domain heterodimer containing the cancer-associated HER3-E909G mutation | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Littlefield, P, Liu, L, Jura, N. | | 登録日 | 2014-10-07 | | 公開日 | 2014-12-10 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.981 Å) | | 主引用文献 | Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations.
Sci.Signal., 7, 2014
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4RIX
 | | Crystal structure of an EGFR/HER3 kinase domain heterodimer containing the cancer-associated HER3-Q790R mutation | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Littlefield, P, Liu, L, Jura, N. | | 登録日 | 2014-10-07 | | 公開日 | 2014-12-10 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations.
Sci.Signal., 7, 2014
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4RIW
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4RIO
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4RG0
 | | Crystal structure of BTK kinase domain complexed with 2-[8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)-2-pyridyl]amino]-6-oxo-3-pyridyl]phenyl]-1-oxo-3,4-dihydroisoquinolin-6-yl]-2-methyl-propanenitrile | | 分子名称: | 2-{8-fluoro-2-[2-(hydroxymethyl)-3-(1-methyl-5-{[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino}-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxo-1,2,3,4-tetrahydroisoquinolin-6-yl}-2-methylpropanenitrile, Tyrosine-protein kinase BTK | | 著者 | Kuglstatter, A, Wong, A. | | 登録日 | 2014-09-29 | | 公開日 | 2014-12-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Bioorg.Med.Chem.Lett., 25, 2015
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4RFZ
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4RFY
 | | Crystal structure of BTK kinase domain complexed with 6-(dimethylamino)-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(morpholine-4-carbonyl)-2-pyridyl]amino]-6-oxo-3-pyridyl]phenyl]-3,4-dihydroisoquinolin-1-one | | 分子名称: | 6-(dimethylamino)-2-[2-(hydroxymethyl)-3-(1-methyl-5-{[5-(morpholin-4-ylcarbonyl)pyridin-2-yl]amino}-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-3,4-dihydroisoquinolin-1(2H)-one, DIMETHYL SULFOXIDE, Tyrosine-protein kinase BTK | | 著者 | Kuglstatter, A, Wong, A. | | 登録日 | 2014-09-29 | | 公開日 | 2014-12-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Bioorg.Med.Chem.Lett., 25, 2015
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4RFM
 | | ITK kinase domain in complex with compound 1 N-{1-[(1,1-dioxo-1-thian-2-yl)(phenyl)methyl]-1H- pyrazol-4-yl}-5,5-difluoro-5a-methyl-1H,4H,4aH,5H,5aH,6H-cyclopropa[f]indazole-3-carboxamide | | 分子名称: | (4aS,5aR)-N-{1-[(R)-[(2R)-1,1-dioxidotetrahydro-2H-thiopyran-2-yl](phenyl)methyl]-1H-pyrazol-4-yl}-5,5-difluoro-5a-methyl-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazole-3-carboxamide, Tyrosine-protein kinase ITK/TSK | | 著者 | McEwan, P.A, Barker, J.J, Eigenbrot, C. | | 登録日 | 2014-09-26 | | 公開日 | 2015-04-29 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
J.Med.Chem., 58, 2015
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4R7I
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4R7H
 | | Crystal structure of FMS KINASE domain with a small molecular inhibitor, PLX3397 | | 分子名称: | 5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-{[6-(trifluoromethyl)pyridin-3-yl]methyl}pyridin-2-amine, Macrophage colony-stimulating factor 1 receptor | | 著者 | Zhang, Y, Zhang, K, Zhang, C. | | 登録日 | 2014-08-27 | | 公開日 | 2015-08-12 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8001 Å) | | 主引用文献 | Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
N Engl J Med, 373, 2015
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4R6V
 | | Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex with FIIN-3, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR kinase Gate-Keeper Mutations | | 分子名称: | Fibroblast growth factor receptor 4, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide, SULFATE ION | | 著者 | Huang, Z, Mohammadi, M. | | 登録日 | 2014-08-26 | | 公開日 | 2014-10-29 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.353 Å) | | 主引用文献 | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4R5Y
 | | The complex structure of Braf V600E kinase domain with a novel Braf inhibitor | | 分子名称: | 5-({(1R,1aS,6bR)-1-[5-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl}oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one, Serine/threonine-protein kinase B-raf | | 著者 | Feng, Y, Peng, H, Zhang, Y, Liu, Y, Wei, M. | | 登録日 | 2014-08-22 | | 公開日 | 2016-02-24 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.5 Å) | | 主引用文献 | BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers.
Mol.Cancer Ther., 14, 2015
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4R5S
 | | Crystal structure of EGFR 696-1022 L858R in complex with FIIN-3 | | 分子名称: | Epidermal growth factor receptor, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide | | 著者 | Zhu, S.J, Yun, C.H. | | 登録日 | 2014-08-22 | | 公開日 | 2014-11-12 | | 最終更新日 | 2022-08-24 | | 実験手法 | X-RAY DIFFRACTION (3.001 Å) | | 主引用文献 | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4R3R
 | | Crystal structures of EGFR in complex with Mig6 | | 分子名称: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1' | | 著者 | Park, E, Kim, N, Yi, Z, Cho, A, Kim, K, Ficarro, S.B, Park, A, Park, W.Y, Murray, B, Meyerson, M, Beroukim, R, Marto, J.A, Cho, J, Eck, M.J. | | 登録日 | 2014-08-17 | | 公開日 | 2015-08-12 | | 最終更新日 | 2015-09-16 | | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | | 主引用文献 | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.
Nat.Struct.Mol.Biol., 22, 2015
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4R3P
 | | Crystal structures of EGFR in complex with Mig6 | | 分子名称: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1 | | 著者 | Park, E, Kim, N, Yi, Z, Cho, A, Kim, K, Ficarro, S.B, Park, A, Park, W.Y, Murray, B, Meyerson, M, Beroukim, R, Marto, J.A, Cho, J, Eck, M.J. | | 登録日 | 2014-08-17 | | 公開日 | 2015-08-12 | | 最終更新日 | 2015-09-16 | | 実験手法 | X-RAY DIFFRACTION (2.905 Å) | | 主引用文献 | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.
Nat.Struct.Mol.Biol., 22, 2015
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4R1Y
 | | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitor | | 分子名称: | 2-(2-(2-(2-(2-(2-ETHOXYETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHANOL, 3-(diethylamino)propyl (3-{[5-(3,4-dimethoxyphenyl)-2-oxo-2H-1,3,4-thiadiazin-3(6H)-yl]methyl}phenyl)carbamate, Hepatocyte growth factor receptor | | 著者 | Blaukat, A, Bladt, F, Friese-Hamim, M, Knuehl, C, Fittschen, C, Graedler, U, Meyring, M, Dorsch, D, Stieber, F, Schadt, O. | | 登録日 | 2014-08-08 | | 公開日 | 2015-03-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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4R1V
 | | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors | | 分子名称: | 3-[1-(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}benzyl)-6-oxo-1,6-dihydropyridazin-3-yl]benzonitrile, GAMMA-BUTYROLACTONE, Hepatocyte growth factor receptor | | 著者 | Blaukat, A, Bladt, F, Friese-Hamim, M, Knuehl, C, Fittschen, C, Graedler, U, Meyring, M, Dorsch, D, Stieber, F, Schadt, O. | | 登録日 | 2014-08-07 | | 公開日 | 2015-03-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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4QT1
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4QRC
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4QQT
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4QQJ
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4QQC
 | | Crystal Structure of FGF Receptor (FGFR) 4 Kinase Domain in Complex with FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations | | 分子名称: | Fibroblast growth factor receptor 4, N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide, SULFATE ION | | 著者 | Huang, Z, Mohammadi, M. | | 登録日 | 2014-06-27 | | 公開日 | 2014-10-29 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4QQ5
 | | Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex With FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations | | 分子名称: | Fibroblast growth factor receptor 4, N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide | | 著者 | Huang, Z, Mohammadi, M. | | 登録日 | 2014-06-26 | | 公開日 | 2014-10-29 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.203 Å) | | 主引用文献 | DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors.
Acs Chem.Biol., 10, 2015
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4QPS
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