3A4O
 
 | | Lyn kinase domain | | 分子名称: | STAUROSPORINE, Tyrosine-protein kinase Lyn | | 著者 | Miyano, N, Kinoshita, T, Tada, T. | | 登録日 | 2009-07-11 | | 公開日 | 2009-12-08 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structural basis for the inhibitor recognition of human Lyn kinase domain
Bioorg.Med.Chem.Lett., 19, 2009
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3AD5
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6J6M
 | | Co-crystal structure of BTK kinase domain with Zanubrutinib | | 分子名称: | (7S)-2-(4-phenoxyphenyl)-7-(1-propanoylpiperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, IMIDAZOLE, Tyrosine-protein kinase BTK | | 著者 | Zhou, X, Hong, Y. | | 登録日 | 2019-01-15 | | 公開日 | 2019-10-23 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.25 Å) | | 主引用文献 | Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
J.Med.Chem., 62, 2019
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7JYS
 | | hALK in complex with 3-(3-chlorophenyl)-5-methyl-1H-pyrazole | | 分子名称: | 1,2-ETHANEDIOL, 3-(3-chlorophenyl)-5-methyl-1H-pyrazole, ALK tyrosine kinase receptor | | 著者 | McGrath, A.P, Zou, H, Lane, W, Saikatendu, K. | | 登録日 | 2020-08-31 | | 公開日 | 2021-01-20 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | Discovery of Novel and Highly Selective Cyclopropane ALK Inhibitors through a Fragment-Assisted, Structure-Based Drug Design.
Acs Omega, 5, 2020
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6GQQ
 | | Crystal structure of human KDR (VEGFR2) kinase domain in complex with AZD3229-analogue (compound 35) | | 分子名称: | Vascular endothelial growth factor receptor 2, ~{N}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(4-propan-2-yl-1,2,3-triazol-1-yl)ethanamide | | 著者 | Schimpl, M, Hardy, C.J, Ogg, D.J, Overman, R.C, Packer, M.J, Kettle, J.G, Anjum, R, Barry, E, Bhavsar, D, Brown, C, Campbell, A, Goldberg, K, Grondine, M, Guichard, S, Hunt, T, Jones, O, Li, X, Moleva, O, Pearson, S, Shao, W, Smith, A, Smith, J, Stead, D, Stokes, S, Tucker, M, Ye, Y. | | 登録日 | 2018-06-07 | | 公開日 | 2018-09-19 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.52 Å) | | 主引用文献 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
J. Med. Chem., 61, 2018
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2YIY
 | | Crystal structure of compound 8 bound to TAK1-TAB | | 分子名称: | (1E)-1-[5-TERT-BUTYL-2-(3-FLUOROPHENYL)-1H-PYRAZOL-3-YLIDENE]-3-(4-PYRIDIN-3-YLOXYPHENYL)UREA, MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE 7, TGF-BETA-ACTIVATED KINASE 1 AND MAP3K7-BINDING PROTEIN 1 | | 著者 | Brown, D.G, Phillips, C. | | 登録日 | 2011-05-17 | | 公開日 | 2012-05-23 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | The Discovery and Synthesis of Selective Dfg-Out Tak-1 Inhibitors
To be Published
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6HD4
 | | ABL1 IN COMPLEX WITH COMPOUND 7 AND IMATINIB (STI-571) | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, 6-[(3~{R})-3-oxidanylpyrrolidin-1-yl]-5-pyrimidin-5-yl-~{N}-[4-(trifluoromethyloxy)phenyl]pyridine-3-carboxamide, CHLORIDE ION, ... | | 著者 | Cowan-Jacob, S.W. | | 登録日 | 2018-08-17 | | 公開日 | 2018-10-24 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.03 Å) | | 主引用文献 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
J. Med. Chem., 61, 2018
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6HES
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with the NVP-BHG712 derivative AT050 | | 分子名称: | 1,2-ETHANEDIOL, 4-methyl-3-[(2-pyridin-3-ylquinazolin-4-yl)amino]-~{N}-[3-(trifluoromethyl)phenyl]benzamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Troester, A, Witt, K, Linhard, V.L, Gande, S.L, Saxena, K, Schwalbe, H. | | 登録日 | 2018-08-20 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.128 Å) | | 主引用文献 | Effects of NVP-BHG712 chemical modifications on EPHA2 binding and affinity
To Be Published
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6HEX
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with the NVP-BHG712 derivative ATMM006 | | 分子名称: | 4-methyl-3-[(1-methyl-6-pyrazin-2-yl-pyrazolo[3,4-d]pyrimidin-4-yl)amino]-~{N}-[3-(trifluoromethyl)phenyl]benzamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Troester, A, Witt, K, Linhard, V.L, Gande, S.L, Saxena, K, Schwalbe, H. | | 登録日 | 2018-08-20 | | 公開日 | 2019-08-28 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.413 Å) | | 主引用文献 | Effects of NVP-BHG712 chemical modifications on EPHA2 binding and affinity
To Be Published
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6HRP
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3BCE
 | | Crystal structure of the ErbB4 kinase | | 分子名称: | DI(HYDROXYETHYL)ETHER, MANGANESE (II) ION, Receptor tyrosine-protein kinase erbB-4, ... | | 著者 | Qiu, C. | | 登録日 | 2007-11-12 | | 公開日 | 2008-02-12 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Mechanism of Activation and Inhibition of the HER4/ErbB4 Kinase.
Structure, 16, 2008
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7KPL
 | | Crystal structure of hEphB1 in apo form | | 分子名称: | Ephrin type-B receptor 1 | | 著者 | Ahmed, M, Wang, P, Sadek, H. | | 登録日 | 2020-11-11 | | 公開日 | 2021-03-10 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.705 Å) | | 主引用文献 | Identification of tetracycline combinations as EphB1 tyrosine kinase inhibitors for treatment of neuropathic pain.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7KPM
 | | Crystal structure of hEphB1 bound with ADP | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Ephrin type-B receptor 1 | | 著者 | Ahmed, M, Wang, P, Sadek, H. | | 登録日 | 2020-11-11 | | 公開日 | 2021-03-10 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (1.608 Å) | | 主引用文献 | Identification of tetracycline combinations as EphB1 tyrosine kinase inhibitors for treatment of neuropathic pain.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7JYT
 | | hALK in complex with 3-(3-methyl-1H-pyrazol-5-yl)pyridine | | 分子名称: | 3-(3-methyl-1H-pyrazol-5-yl)pyridine, ALK tyrosine kinase receptor, GLYCEROL | | 著者 | McGrath, A.P, Zou, H, Lane, W, Saikatendu, K. | | 登録日 | 2020-08-31 | | 公開日 | 2021-01-20 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery of Novel and Highly Selective Cyclopropane ALK Inhibitors through a Fragment-Assisted, Structure-Based Drug Design.
Acs Omega, 5, 2020
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2YJS
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2YN8
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7JY4
 | | hALK in complex with ((1S,2S)-1-(2,4-difluorophenyl)-2-(2-(3-methyl-1H-pyrazol-5-yl)-4-(trifluoromethyl)phenoxy)cyclopropyl)methanamine | | 分子名称: | 1-{(1S,2S)-1-(2,4-difluorophenyl)-2-[2-(3-methyl-1H-pyrazol-5-yl)-4-(trifluoromethyl)phenoxy]cyclopropyl}methanamine, ALK tyrosine kinase receptor | | 著者 | McGrath, A.P, Zou, H, Lane, W, Saikatendu, K. | | 登録日 | 2020-08-28 | | 公開日 | 2021-01-20 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.42 Å) | | 主引用文献 | Discovery of Novel and Highly Selective Cyclopropane ALK Inhibitors through a Fragment-Assisted, Structure-Based Drug Design.
Acs Omega, 5, 2020
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3B8Q
 | | Crystal structure of the VEGFR2 kinase domain in complex with a naphthamide inhibitor | | 分子名称: | N-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide, Vascular endothelial growth factor receptor 2 | | 著者 | Whittington, D.A, Long, A.M, Gu, Y, Zhao, H. | | 登録日 | 2007-11-01 | | 公開日 | 2008-04-01 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | | 主引用文献 | Naphthamides as Novel and Potent Vascular Endothelial Growth Factor
Receptor Tyrosine Kinase Inhibitors: Design, Synthesis and Evaluation
J.Med.Chem., 51, 2008
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3B2T
 | | Structure of phosphotransferase | | 分子名称: | 5'-O-[(S)-hydroxy{[(S)-hydroxy(methyl)phosphoryl]oxy}phosphoryl]adenosine, Fibroblast growth factor receptor 2, PHOSPHATE ION | | 著者 | Lew, E.D, Bae, J.H, Rohmann, E, Wollnik, B, Schlessinger, J. | | 登録日 | 2007-10-19 | | 公開日 | 2008-02-26 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structural basis for reduced FGFR2 activity in LADD syndrome: Implications for FGFR autoinhibition and activation.
Proc.Natl.Acad.Sci.Usa, 104, 2007
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3BEA
 | | cFMS tyrosine kinase (tie2 KID) in complex with a pyrimidinopyridone inhibitor | | 分子名称: | 8-(2,3-dihydro-1H-inden-5-yl)-2-({4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]phenyl}amino)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, Macrophage colony-stimulating factor 1 receptor, SULFATE ION | | 著者 | Schubert, C. | | 登録日 | 2007-11-16 | | 公開日 | 2008-07-15 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Bioorg.Med.Chem.Lett., 18, 2008
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7JU6
 | | Structure of RET protein tyrosine kinase in complex with selpercatinib | | 分子名称: | FORMIC ACID, Proto-oncogene tyrosine-protein kinase receptor Ret, Selpercatinib | | 著者 | Terzyan, S.S, Shen, T, Wu, J, Mooers, B.H.M. | | 登録日 | 2020-08-19 | | 公開日 | 2020-11-11 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.06 Å) | | 主引用文献 | Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations.
Ann Oncol, 32, 2021
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3BBW
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6HMX
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2Z8C
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2ZV7
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