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 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Insulin, ... | Authors: | Zhang, X, Yu, D, Wang, T. | Deposit date: | 2019-02-27 | Release date: | 2020-03-04 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (4.7 Å) | Cite: | 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 | Descriptor: | (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 | Authors: | Zhou, X, Hong, Y. | Deposit date: | 2019-01-15 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.25 Å) | Cite: | 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 | Descriptor: | 2'-DEOXYADENOSINE 5'-TRIPHOSPHATE, Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, ... | Authors: | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | Deposit date: | 2019-01-15 | Release date: | 2019-03-20 | Last modified: | 2023-04-12 | Method: | ELECTRON MICROSCOPY (3.7 Å) | Cite: | 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 | Descriptor: | Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, Protein kinase superfamily protein, ... | Authors: | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | Deposit date: | 2019-01-12 | Release date: | 2019-04-03 | Last modified: | 2024-10-16 | Method: | ELECTRON MICROSCOPY (4.25 Å) | Cite: | 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 | Descriptor: | Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, Protein kinase superfamily protein, ... | Authors: | Wang, J.Z, Wang, J, Meijuan, H, Wang, H.W, Zhou, J.M, Chai, J.J. | Deposit date: | 2019-01-12 | Release date: | 2019-04-03 | Last modified: | 2023-04-05 | Method: | ELECTRON MICROSCOPY (3.9 Å) | Cite: | 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 | Descriptor: | 2'-DEOXYADENOSINE 5'-TRIPHOSPHATE, Disease resistance RPP13-like protein 4, Probable serine/threonine-protein kinase PBL2, ... | Authors: | Wang, J.Z, Wang, J, Hu, M.J, Wang, H.W, Zhou, J.M, Chai, J.J. | Deposit date: | 2019-01-12 | Release date: | 2019-03-20 | Last modified: | 2024-10-16 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Xu, Y, Liu, Q. | Deposit date: | 2018-11-29 | Release date: | 2019-11-06 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Xu, Y, Liu, Q. | Deposit date: | 2018-11-29 | Release date: | 2019-10-23 | Last modified: | 2024-10-16 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Wu, T.S, Wu, S.Y. | Deposit date: | 2018-11-26 | Release date: | 2019-11-27 | Method: | X-RAY DIFFRACTION (1.881 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Wu, T.S, Wu, S.Y. | Deposit date: | 2018-11-26 | Release date: | 2019-11-27 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.103 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Xu, Y, Liu, Q. | Deposit date: | 2018-11-23 | Release date: | 2019-10-23 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.994 Å) | Cite: | 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 | Descriptor: | 4-[[4-azanyl-3-(4-cyclohexylpiperazin-1-yl)-9,10-bis(oxidanylidene)anthracen-1-yl]amino]benzoic acid, High affinity nerve growth factor receptor | Authors: | Noritaka, F. | Deposit date: | 2018-11-08 | Release date: | 2020-01-22 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.54 Å) | Cite: | 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 | Descriptor: | 1,4,7,10,13,16-HEXAOXACYCLOOCTADECANE, CHLORIDE ION, Ephrin type-A receptor 3 | Authors: | Yokoyama, T, Kosaka, Y, Matsumoto, K, Kitakami, R, Nabeshima, Y, Mizuguchi, M. | Deposit date: | 2018-10-24 | Release date: | 2019-10-30 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (1.501 Å) | Cite: | Crown Ethers as Transthyretin Amyloidogenesis Inhibitor To Be Published
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6IL3
| Crystal structure of the FLT3 kinase bound to a small molecule inhibitor | Descriptor: | 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, 7-methoxy-6-(1-methyl-1H-pyrazol-4-yl)-3-(pyridin-2-yl)imidazo[1,2-a]pyridine, CHLORIDE ION, ... | Authors: | Thomas, C.J. | Deposit date: | 2018-10-16 | Release date: | 2018-12-12 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Crystal structure of the FLT3 kinase bound to a small molecule inhibitor To Be Published
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6IG8
| Crystal structure of CSF-1R kinase domain with a small molecular inhibitor, JTE-952 | Descriptor: | (3-{4-[(4-cyclopropylphenyl)methoxy]-3-methoxyphenyl}azetidin-1-yl)(4-{[(2S)-2,3-dihydroxypropoxy]methyl}pyridin-2-yl)methanone, GLYCEROL, MAGNESIUM ION, ... | Authors: | Doi, S, Adachi, T. | Deposit date: | 2018-09-25 | Release date: | 2019-08-07 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | Sousa, B.B, Matias, P.M, Marques, M.C, Seixas, J.D, Bernardes, G.J.L. | Deposit date: | 2018-11-22 | Release date: | 2020-05-27 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.001 Å) | Cite: | 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. | Descriptor: | 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 | Authors: | Bader, G, Zoephel, A. | Deposit date: | 2018-11-21 | Release date: | 2019-02-20 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (1.99 Å) | Cite: | Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J.Med.Chem., 62, 2019
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6I83
| Crystal structure of phosphorylated RET V804M tyrosine kinase domain complexed with PDD00018366 | Descriptor: | 4-[5-(pyridin-3-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide, FORMIC ACID, Proto-oncogene tyrosine-protein kinase receptor Ret | Authors: | Burschowsky, D, Seewooruthun, C, Bayliss, R, Carr, M.D, Echalier, A, Jordan, A.M. | Deposit date: | 2018-11-19 | Release date: | 2020-03-11 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (1.88 Å) | Cite: | Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804MKinase. Acs Med.Chem.Lett., 11, 2020
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6I82
| Crystal structure of partially phosphorylated RET V804M tyrosine kinase domain complexed with PDD00018412 | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, FORMIC ACID, ... | Authors: | Burschowsky, D, Seewooruthun, C, Bayliss, R, Carr, M.D, Echalier, A, Jordan, A.M. | Deposit date: | 2018-11-19 | Release date: | 2020-03-11 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804MKinase. Acs Med.Chem.Lett., 11, 2020
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6HZV
| HUMAN JAK3 IN COMPLEX WITH LASW959 PROTEIN IN COMPLEX WITH LIGAND | Descriptor: | 3-[7-(2-hydroxyethyl)-9-(oxan-4-yl)-8-oxidanylidene-purin-2-yl]imidazo[1,2-a]pyridine-6-carbonitrile, Tyrosine-protein kinase JAK3 | Authors: | Lozoya, E, Segarra, V, Bach, J, Jestel, A, Lammens, A, Blaesse, M. | Deposit date: | 2018-10-24 | Release date: | 2019-10-23 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.46 Å) | Cite: | Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases. J.Med.Chem., 62, 2019
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6HZU
| HUMAN JAK1 IN COMPLEX WITH LASW1393 | Descriptor: | 2-[4-[8-oxidanylidene-2-[(~{E})-(2-oxidanylidenepyridin-3-ylidene)amino]-7~{H}-purin-9-yl]cyclohexyl]ethanenitrile, Tyrosine-protein kinase JAK1 | Authors: | Lozoya, E, Segarra, V, Bach, J, Jestel, A, Lammens, A, Blaesse, M. | Deposit date: | 2018-10-24 | Release date: | 2019-10-23 | Last modified: | 2024-10-09 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases. J.Med.Chem., 62, 2019
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6HVF
| Kinase domain of cSrc in complex with compound 29B | Descriptor: | 1,2-ETHANEDIOL, Proto-oncogene tyrosine-protein kinase Src, ~{N}-[3-[3-ethyl-6-[4-(4-methylpiperazin-1-yl)phenyl]-4-oxidanylidene-7~{H}-pyrrolo[2,3-d]pyrimidin-5-yl]phenyl]prop-2-enamide | Authors: | Keul, M, Mueller, M.P, Rauh, D. | Deposit date: | 2018-10-10 | Release date: | 2019-10-23 | Last modified: | 2020-01-01 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S. Chem Sci, 10, 2019
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