4R3R
| Crystal structures of EGFR in complex with Mig6 | Descriptor: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1' | Authors: | 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. | Deposit date: | 2014-08-17 | Release date: | 2015-08-12 | Last modified: | 2015-09-16 | Method: | X-RAY DIFFRACTION (3.25 Å) | Cite: | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6. Nat.Struct.Mol.Biol., 22, 2015
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3CPB
| Crystal structure of the VEGFR2 kinase domain in complex with a bisamide inhibitor | Descriptor: | N'-(6-aminopyridin-3-yl)-N-(2-cyclopentylethyl)-4-methyl-benzene-1,3-dicarboxamide, Vascular endothelial growth factor receptor 2 | Authors: | Whittington, D.A, Long, A.M, Rose, P, Gu, Y, Zhao, H. | Deposit date: | 2008-03-31 | Release date: | 2008-06-17 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit. J.Med.Chem., 51, 2008
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4R5S
| Crystal structure of EGFR 696-1022 L858R in complex with FIIN-3 | Descriptor: | 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 | Authors: | Zhu, S.J, Yun, C.H. | Deposit date: | 2014-08-22 | Release date: | 2014-11-12 | Last modified: | 2022-08-24 | Method: | X-RAY DIFFRACTION (3.001 Å) | Cite: | 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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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 | Descriptor: | (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 | Authors: | McEwan, P.A, Barker, J.J, Eigenbrot, C. | Deposit date: | 2014-09-26 | Release date: | 2015-04-29 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | 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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5A46
| FGFR1 in complex with dovitinib | Descriptor: | 1,2-ETHANEDIOL, 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | Authors: | Klein, T, Vajpai, N, Phillips, J.J, Davies, G, Holdgate, G.A, Phillips, C, Tucker, J.A, Norman, R.A, Scott, A.S, Higazi, D.R, Lowe, D, Thompson, G.S, Breeze, A.L. | Deposit date: | 2015-06-05 | Release date: | 2015-08-05 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.63 Å) | Cite: | Structural and Dynamic Insights Into the Energetics of Activation Loop Rearrangement in Fgfr1 Kinase. Nat.Commun., 6, 2015
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4R7I
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4RFZ
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4DFN
| Crystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitor | Descriptor: | 3-amino-6-[3-(1-methyl-1H-pyrazol-4-yl)phenyl]-N-[(1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl]pyrazine-2-carboxamide, Tyrosine-protein kinase SYK | Authors: | Lopez, M, Segarra, V, Vidal, B, Wenzkowski, C, Jestel, A, Krapp, S, Blaesse, M, Nagel, S, Schreiner, P. | Deposit date: | 2012-01-24 | Release date: | 2012-04-25 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.48 Å) | Cite: | Pyrazine-based Syk kinase inhibitors. Bioorg.Med.Chem.Lett., 22, 2012
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4BBF
| Aminoalkylpyrimidine Inhibitor Complexes with JAK2 | Descriptor: | (2R)-N-[4-[2-[(4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide, TYROSINE-PROTEIN KINASE JAK2 | Authors: | Li, J. | Deposit date: | 2012-09-21 | Release date: | 2012-11-21 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Sar and in Vivo Evaluation of 4-Aryl-2-Aminoalkylpyrimidines as Potent and Selective Janus Kinase 2 (Jak2) Inhibitors Bioorg.Med.Chem.Lett., 22, 2012
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5C8N
| EGFR kinase domain mutant "TMLR" with compound 23 | Descriptor: | Epidermal growth factor receptor, N-{2-[4-(2-aminoethyl)-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-2-methyl-1-(propan-2-yl)-1H-imidazo[4,5-c]pyridin-6-amine, SULFATE ION | Authors: | Eigenbrot, C, Yu, C. | Deposit date: | 2015-06-25 | Release date: | 2015-10-28 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.401 Å) | Cite: | Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study. J.Med.Chem., 58, 2015
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5BVN
| Fragment-based discovery of potent and selective DDR1/2 inhibitors | Descriptor: | Epithelial discoidin domain-containing receptor 1, IODIDE ION, N-[5-({[(3-fluorophenyl)carbamoyl]amino}methyl)-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide | Authors: | Murray, C, Berdini, V, Buck, I, Carr, M, Cleasby, A, Coyle, J, Curry, J, Day, J, Hearn, K, Iqbal, A, Lee, L, Martins, V, Mortenson, P, Munck, J, Page, L, Patel, S, Roomans, S, Kirsten, T, Saxty, G. | Deposit date: | 2015-06-05 | Release date: | 2015-08-12 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.21 Å) | Cite: | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. Acs Med.Chem.Lett., 6, 2015
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5C26
| Crystal structure of SYK in complex with compound 1 | Descriptor: | 3-{8-[(3,4-dimethoxyphenyl)amino]imidazo[1,2-a]pyrazin-6-yl}benzamide, GLU-VAL-PTR-GLU-SER-PRO, Tyrosine-protein kinase SYK | Authors: | Han, S, Chang, J. | Deposit date: | 2015-06-15 | Release date: | 2015-10-07 | Last modified: | 2016-02-03 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free-Energy Perturbation (FEP). Chemmedchem, 11, 2016
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3DQW
| c-Src kinase domain Thr338Ile mutant in complex with ATPgS | Descriptor: | MAGNESIUM ION, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, Proto-oncogene tyrosine-protein kinase Src | Authors: | Azam, M, Seeliger, M.A, Gray, N, Kuriyan, J, Daley, G.Q. | Deposit date: | 2008-07-09 | Release date: | 2008-09-23 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.017 Å) | Cite: | Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat.Struct.Mol.Biol., 15, 2008
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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 | Descriptor: | 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 | Authors: | Kuglstatter, A, Wong, A. | Deposit date: | 2014-09-29 | Release date: | 2014-12-24 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | 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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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 | Descriptor: | 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 | Authors: | Huang, Z, Mohammadi, M. | Deposit date: | 2014-06-27 | Release date: | 2014-10-29 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | 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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3DK3
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3DKG
| Structure of Mutant(Y1248L) MET receptor tyrosine kinase in complex with inhibitor SGX-523 | Descriptor: | 6-{[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}quinoline, CHLORIDE ION, Hepatocyte growth factor receptor | Authors: | Hendle, J. | Deposit date: | 2008-06-24 | Release date: | 2009-07-07 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.91 Å) | Cite: | SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol.Cancer Ther., 8, 2009
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3DPK
| cFMS tyrosine kinase in complex with a pyridopyrimidinone inhibitor | Descriptor: | 8-cyclohexyl-N-methoxy-5-oxo-2-{[4-(2-pyrrolidin-1-ylethyl)phenyl]amino}-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, Macrophage colony-stimulating factor 1 receptor, Fibroblast growth factor receptor 1, ... | Authors: | Schubert, C. | Deposit date: | 2008-07-08 | Release date: | 2009-02-17 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors J.Med.Chem., 52, 2009
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3F82
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3F3W
| Drug resistant cSrc kinase domain in complex with inhibitor RL45 (Type II) | Descriptor: | 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 | Authors: | Grutter, C, Kluter, S, Getlik, M, Rauh, D. | Deposit date: | 2008-10-31 | Release date: | 2009-06-02 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc J.Med.Chem., 52, 2009
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4QPS
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3F6X
| c-Src kinase domain in complex with small molecule inhibitor | Descriptor: | Proto-oncogene tyrosine-protein kinase Src, [4-({4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]quinazolin-2-yl}amino)phenyl]acetonitrile | Authors: | Seeliger, M.A, Statsuk, A.V, Maly, D.J, Patrick, P.Z, Kuriyan, J, Shokat, K.M. | Deposit date: | 2008-11-06 | Release date: | 2008-12-09 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Tuning a three-component reaction for trapping kinase substrate complexes. J.Am.Chem.Soc., 130, 2008
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4R5Y
| The complex structure of Braf V600E kinase domain with a novel Braf inhibitor | Descriptor: | 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 | Authors: | Feng, Y, Peng, H, Zhang, Y, Liu, Y, Wei, M. | Deposit date: | 2014-08-22 | Release date: | 2016-02-24 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (3.5 Å) | Cite: | 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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4D2R
| Human IGF in complex with a Dyrk1B inhibitor | Descriptor: | CHLORIDE ION, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR, N-{2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine | Authors: | Debreczeni, J.E, Kettle, J.G, Ballard, P, Bardelle, C, Butterworth, S, Colclough, N, Critchlow, S.E, Fairley, G, Fillery, S, Graham, M.A, Goodwin, L, Guichard, S, Hudson, K, Mahmood, A, Vincent, J, Ward, R.A, Whittaker, D. | Deposit date: | 2014-05-12 | Release date: | 2015-04-22 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors to Explore a Mek Resistance Hypothesis. J.Med.Chem., 58, 2015
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4ZLZ
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