6JPJ
 
 | | Crystal structure of FGF401 in complex of FGFR4 | | 分子名称: | Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-methanoyl-6-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide, SULFATE ION | | 著者 | Zhou, Z, Chen, X, Chen, Y. | | 登録日 | 2019-03-27 | | 公開日 | 2019-05-15 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.638 Å) | | 主引用文献 | Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4.
Chem.Commun.(Camb.), 55, 2019
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6JPE
 | | Crystal structure of FGFR4 kinase domain with irreversible inhibitor 1 | | 分子名称: | Fibroblast growth factor receptor 4, N-[2-[[6-[2-[[2,6-bis(chloranyl)-3,5-dimethoxy-phenyl]amino]pyridin-3-yl]pyrimidin-4-yl]amino]-3-methyl-phenyl]prop-2-enamide, SULFATE ION | | 著者 | Chen, X, Dai, S, Zhou, Z, Chen, Y. | | 登録日 | 2019-03-26 | | 公開日 | 2020-05-06 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.601 Å) | | 主引用文献 | Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma.
J.Med.Chem., 63, 2020
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6JOL
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6JOK
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6JOJ
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6JOI
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6JMF
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6JK8
 | | Cryo-EM structure of the full-length human IGF-1R in complex with insulin | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Insulin, ... | | 著者 | Zhang, X, Yu, D, Wang, T. | | 登録日 | 2019-02-27 | | 公開日 | 2020-03-04 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (4.7 Å) | | 主引用文献 | Visualization of Ligand-Bound Ectodomain Assembly in the Full-Length Human IGF-1 Receptor by Cryo-EM Single-Particle Analysis.
Structure, 28, 2020
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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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6J6I
 | | Reconstitution and structure of a plant NLR resistosome conferring immunity | | 分子名称: | 2'-DEOXYADENOSINE 5'-TRIPHOSPHATE, Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, ... | | 著者 | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | | 登録日 | 2019-01-15 | | 公開日 | 2019-03-20 | | 最終更新日 | 2023-04-12 | | 実験手法 | ELECTRON MICROSCOPY (3.7 Å) | | 主引用文献 | Reconstitution and structure of a plant NLR resistosome conferring immunity.
Science, 364, 2019
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6J5V
 | | Ligand-triggered allosteric ADP release primes a plant NLR complex | | 分子名称: | Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, Protein kinase superfamily protein, ... | | 著者 | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | | 登録日 | 2019-01-12 | | 公開日 | 2019-04-03 | | 最終更新日 | 2023-04-05 | | 実験手法 | ELECTRON MICROSCOPY (4.25 Å) | | 主引用文献 | Ligand-triggered allosteric ADP release primes a plant NLR complex.
Science, 364, 2019
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6J5U
 | | Ligand-triggered allosteric ADP release primes a plant NLR complex | | 分子名称: | Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, Protein kinase superfamily protein, ... | | 著者 | Wang, J.Z, Wang, J, Meijuan, H, Wang, H.W, Zhou, J.M, Chai, J.J. | | 登録日 | 2019-01-12 | | 公開日 | 2019-04-03 | | 最終更新日 | 2023-04-05 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Ligand-triggered allosteric ADP release primes a plant NLR complex.
Science, 364, 2019
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6J5T
 | | Reconstitution and structure of a plant NLR resistosome conferring immunity | | 分子名称: | 2'-DEOXYADENOSINE 5'-TRIPHOSPHATE, Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, ... | | 著者 | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | | 登録日 | 2019-01-12 | | 公開日 | 2019-03-20 | | 最終更新日 | 2023-04-12 | | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | | 主引用文献 | Reconstitution and structure of a plant NLR resistosome conferring immunity.
Science, 364, 2019
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6J5L
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6IUP
 | | Crystal structure of FGFR4 kinase domain in complex with compound 5 | | 分子名称: | DIMETHYL SULFOXIDE, Fibroblast growth factor receptor 4, N-{4-[4-amino-3-(3,5-dimethyl-1-benzofuran-2-yl)-7-oxo-6,7-dihydro-2H-pyrazolo[3,4-d]pyridazin-2-yl]phenyl}prop-2-enamide | | 著者 | Xu, Y, Liu, Q. | | 登録日 | 2018-11-29 | | 公開日 | 2019-11-06 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design.
J.Med.Chem., 62, 2019
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6IUO
 | | Crystal structure of FGFR4 kinase domain in complex with a covalent inhibitor | | 分子名称: | Fibroblast growth factor receptor 4, N-({4-[4-amino-3-(3,5-dimethyl-1-benzofuran-2-yl)-7-oxo-6,7-dihydro-2H-pyrazolo[3,4-d]pyridazin-2-yl]phenyl}methyl)prop-2-enamide | | 著者 | Xu, Y, Liu, Q. | | 登録日 | 2018-11-29 | | 公開日 | 2019-10-23 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design.
J.Med.Chem., 62, 2019
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6ITV
 | | Crystal structure of activated c-KIT in complex with compound | | 分子名称: | Mast/stem cell growth factor receptor Kit, N-(5-ethyl-1,2-oxazol-3-yl)-N'-[4-(2-{[6-(4-ethylpyrazin-1(4H)-yl)pyrimidin-4-yl]amino}-1,3-thiazol-5-yl)phenyl]urea | | 著者 | Wu, T.S, Wu, S.Y. | | 登録日 | 2018-11-26 | | 公開日 | 2019-11-27 | | 実験手法 | X-RAY DIFFRACTION (1.881 Å) | | 主引用文献 | Crystal structure of activated c-KIT in complex with compound
To Be Published
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6ITT
 | | Crystal structure of unactivated c-KIT in complex with compound | | 分子名称: | Mast/stem cell growth factor receptor Kit, N-(5-ethyl-1,2-oxazol-3-yl)-N'-[4-(2-{[6-(4-ethylpyrazin-1(4H)-yl)pyrimidin-4-yl]amino}-1,3-thiazol-5-yl)phenyl]urea | | 著者 | Wu, T.S, Wu, S.Y. | | 登録日 | 2018-11-26 | | 公開日 | 2019-11-27 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.103 Å) | | 主引用文献 | Crystal structure of unactivated c-KIT in complex with compound
To Be Published
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6ITJ
 | | Crystal structure of FGFR1 kinase domain in complex with compound 3 | | 分子名称: | 4-azanyl-3-(3,5-dimethyl-1-benzofuran-2-yl)-2-phenyl-6~{H}-pyrazolo[3,4-d]pyridazin-7-one, Fibroblast growth factor receptor 1 | | 著者 | Xu, Y, Liu, Q. | | 登録日 | 2018-11-23 | | 公開日 | 2019-10-23 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.994 Å) | | 主引用文献 | Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design.
J.Med.Chem., 62, 2019
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6IQN
 | | Crystal structure of TrkA kinase with ligand | | 分子名称: | 4-[[4-azanyl-3-(4-cyclohexylpiperazin-1-yl)-9,10-bis(oxidanylidene)anthracen-1-yl]amino]benzoic acid, High affinity nerve growth factor receptor | | 著者 | Noritaka, F. | | 登録日 | 2018-11-08 | | 公開日 | 2020-01-22 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.54 Å) | | 主引用文献 | An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue.
Bioorg.Med.Chem.Lett., 30, 2020
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6IN0
 | | Crystal structure of EphA3 in complex with 18-Crown-6 | | 分子名称: | 1,4,7,10,13,16-HEXAOXACYCLOOCTADECANE, CHLORIDE ION, Ephrin type-A receptor 3 | | 著者 | Yokoyama, T, Kosaka, Y, Matsumoto, K, Kitakami, R, Nabeshima, Y, Mizuguchi, M. | | 登録日 | 2018-10-24 | | 公開日 | 2019-10-30 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (1.501 Å) | | 主引用文献 | Crown Ethers as Transthyretin Amyloidogenesis Inhibitor
To Be Published
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6IL3
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6IG8
 | | Crystal structure of CSF-1R kinase domain with a small molecular inhibitor, JTE-952 | | 分子名称: | (3-{4-[(4-cyclopropylphenyl)methoxy]-3-methoxyphenyl}azetidin-1-yl)(4-{[(2S)-2,3-dihydroxypropoxy]methyl}pyridin-2-yl)methanone, GLYCEROL, MAGNESIUM ION, ... | | 著者 | Doi, S, Adachi, T. | | 登録日 | 2018-09-25 | | 公開日 | 2019-08-07 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by the use of docking models.
Bioorg.Med.Chem.Lett., 29, 2019
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6I99
 | | Bone Marrow Tyrosine Kinase in Chromosome X in complex with a newly designed covalent inhibitor JS24 | | 分子名称: | Cytoplasmic tyrosine-protein kinase BMX, ~{N}-[2-methyl-5-[8-[4-(methylsulfonylamino)phenyl]-2-oxidanylidene-benzo[h][1,6]naphthyridin-1-yl]phenyl]-3-oxidanyl-propanamide | | 著者 | Sousa, B.B, Matias, P.M, Marques, M.C, Seixas, J.D, Bernardes, G.J.L. | | 登録日 | 2018-11-22 | | 公開日 | 2020-05-27 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.001 Å) | | 主引用文献 | Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors
Chem.Biol., 2020
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6I8Z
 | | Crystal structure of PTK2 in complex with BI-4464. | | 分子名称: | 3-methoxy-~{N}-(1-methylpiperidin-1-ium-4-yl)-4-[[4-[(3-oxidanylidene-1,2-dihydroinden-4-yl)oxy]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide, Focal adhesion kinase 1 | | 著者 | Bader, G, Zoephel, A. | | 登録日 | 2018-11-21 | | 公開日 | 2019-02-20 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions.
J.Med.Chem., 62, 2019
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