6DUD
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![BU of 6dud by Molmil](/molmil-images/mine/6dud) | JAK3 with cyanamide CP12 | Descriptor: | N-[(1S)-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]imidoformamide, SULFATE ION, Tyrosine-protein kinase JAK3 | Authors: | Vajdos, F.F. | Deposit date: | 2018-06-20 | Release date: | 2018-11-28 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.66 Å) | Cite: | Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. J. Med. Chem., 61, 2018
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1OPJ
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![BU of 1opj by Molmil](/molmil-images/mine/1opj) | Structural basis for the auto-inhibition of c-Abl tyrosine kinase | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, MYRISTIC ACID, ... | Authors: | Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | Deposit date: | 2003-03-06 | Release date: | 2003-04-08 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Structural basis for the autoinhibition of c-Abl tyrosine kinase Cell(Cambridge,Mass.), 112, 2003
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6DB4
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![BU of 6db4 by Molmil](/molmil-images/mine/6db4) | JAK3 with Cyanamide CP34 | Descriptor: | N-[(1S)-6-(5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]imidoformamide, Tyrosine-protein kinase JAK3 | Authors: | Vajdos, F.F. | Deposit date: | 2018-05-02 | Release date: | 2018-11-28 | Last modified: | 2019-05-01 | Method: | X-RAY DIFFRACTION (1.662 Å) | Cite: | Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. J. Med. Chem., 61, 2018
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6DI5
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![BU of 6di5 by Molmil](/molmil-images/mine/6di5) | CRYSTAL STRUCTURE OF BTK IN COMPLEX WITH COVALENT INHIBITOR | Descriptor: | 2-(4-phenoxyphenoxy)-6-[(1S,4S)-5-propanoyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyridine-3-carboxamide, DIMETHYL SULFOXIDE, Tyrosine-protein kinase BTK | Authors: | Gardberg, A. | Deposit date: | 2018-05-22 | Release date: | 2018-09-05 | Method: | X-RAY DIFFRACTION (1.42 Å) | Cite: | Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. Bioorg. Med. Chem. Lett., 28, 2018
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6DI0
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![BU of 6di0 by Molmil](/molmil-images/mine/6di0) | CRYSTAL STRUCTURE OF BTK IN COMPLEX WITH FRAGMENT LIGAND | Descriptor: | 6-(cyclohexylamino)pyridine-3-carboxamide, Tyrosine-protein kinase BTK | Authors: | MOCHALKIN, I. | Deposit date: | 2018-05-22 | Release date: | 2018-10-17 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.3 Å) | Cite: | Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. Bioorg. Med. Chem. Lett., 28, 2018
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6D8E
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![BU of 6d8e by Molmil](/molmil-images/mine/6d8e) | |
1P4O
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![BU of 1p4o by Molmil](/molmil-images/mine/1p4o) | Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. | Descriptor: | Insulin-like growth factor I receptor protein | Authors: | Munshi, S, Kornienko, M, Hall, D.L, Darke, P.L, Waxman, L, Kuo, L.C. | Deposit date: | 2003-04-23 | Release date: | 2003-04-29 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution. Acta Crystallogr.,Sect.D, 59, 2003
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1OEC
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![BU of 1oec by Molmil](/molmil-images/mine/1oec) | FGFr2 kinase domain | Descriptor: | 4-ARYL-2-PHENYLAMINO PYRIMIDINE, FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION | Authors: | Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J. | Deposit date: | 2003-03-24 | Release date: | 2004-10-27 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | The Crystal Structure of the Fgfr2 Tyrosine Kinase Domain in Complex with 4-Aryl-2-Phenylamino Pyrimidine Angiogenesis Inhibitors To be Published
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1PKG
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![BU of 1pkg by Molmil](/molmil-images/mine/1pkg) | Structure of a c-Kit Kinase Product Complex | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein | Authors: | Mol, C.D, Lim, K.B, Sridhar, V, Zou, H, Chien, E.Y.T, Sang, B.-C, Nowakowski, J, Kassel, D.B, Cronin, C.N, McRee, D.E. | Deposit date: | 2003-06-05 | Release date: | 2003-08-12 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation. J.Biol.Chem., 278, 2003
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1QPD
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![BU of 1qpd by Molmil](/molmil-images/mine/1qpd) | STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS | Descriptor: | LCK KINASE, STAUROSPORINE, SULFATE ION | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A. | Deposit date: | 1999-05-24 | Release date: | 2000-05-24 | Last modified: | 2022-12-21 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors. Structure Fold.Des., 7, 1999
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1P14
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![BU of 1p14 by Molmil](/molmil-images/mine/1p14) | Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase | Descriptor: | insulin receptor | Authors: | Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R. | Deposit date: | 2003-04-11 | Release date: | 2003-07-22 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor J.Biol.Chem., 278, 2003
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1QPE
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1QPJ
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![BU of 1qpj by Molmil](/molmil-images/mine/1qpj) | CRYSTAL STRUCTURE OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH STAUROSPORINE. | Descriptor: | LCK TYROSINE KINASE, STAUROSPORINE, SULFATE ION | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M. | Deposit date: | 1999-05-25 | Release date: | 2000-05-31 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors. Structure Fold.Des., 7, 1999
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1QPC
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![BU of 1qpc by Molmil](/molmil-images/mine/1qpc) | STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS | Descriptor: | 1,2-ETHANEDIOL, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, SULFATE ION, ... | Authors: | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A. | Deposit date: | 1999-05-21 | Release date: | 2000-05-24 | Last modified: | 2015-08-19 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors. Structure Fold.Des., 7, 1999
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1XBA
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![BU of 1xba by Molmil](/molmil-images/mine/1xba) | Crystal structure of apo syk tyrosine kinase domain | Descriptor: | Tyrosine-protein kinase SYK | Authors: | Atwell, S, Adams, J.M, Badger, J, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Nienaber, V.L, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | Deposit date: | 2004-08-30 | Release date: | 2004-11-02 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. J.Biol.Chem., 279, 2004
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1XBB
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![BU of 1xbb by Molmil](/molmil-images/mine/1xbb) | Crystal structure of the syk tyrosine kinase domain with Gleevec | Descriptor: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Tyrosine-protein kinase SYK | Authors: | Nienaber, V.L, Atwell, S, Adams, J.M, Badger, J, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | Deposit date: | 2004-08-30 | Release date: | 2004-11-02 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (1.57 Å) | Cite: | A Novel Mode of Gleevec Binding Is Revealed by the Structure of Spleen Tyrosine Kinase J.Biol.Chem., 279, 2004
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1XBC
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![BU of 1xbc by Molmil](/molmil-images/mine/1xbc) | Crystal structure of the syk tyrosine kinase domain with Staurosporin | Descriptor: | STAUROSPORINE, Tyrosine-protein kinase SYK | Authors: | Badger, J, Atwell, S, Adams, J.M, Buchanan, M.D, Feil, I.K, Froning, K.J, Gao, X, Hendle, J, Keegan, K, Leon, B.C, Muller-Deickmann, H.J, Nienaber, V.L, Noland, B.W, Post, K, Rajashankar, K.R, Ramos, A, Russell, M, Burley, S.K, Buchanan, S.G. | Deposit date: | 2004-08-30 | Release date: | 2004-11-02 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase J.Biol.Chem., 279, 2004
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1XKK
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![BU of 1xkk by Molmil](/molmil-images/mine/1xkk) | EGFR kinase domain complexed with a quinazoline inhibitor- GW572016 | Descriptor: | Epidermal growth factor receptor, N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE, PHOSPHATE ION | Authors: | Wood, E.R, Truesdale, A.T, McDonald, O.B, Yuan, D, Hassell, A, Dickerson, S.H, Ellis, B, Pennisi, C, Horne, E, Lackey, K, Alligood, K.J, Rusnak, D.W, Gilmer, T.M, Shewchuk, L.M. | Deposit date: | 2004-09-29 | Release date: | 2004-12-07 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res., 64, 2004
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1YOL
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![BU of 1yol by Molmil](/molmil-images/mine/1yol) | Crystal structure of Src kinase domain in complex with CGP77675 | Descriptor: | 1-{4-[4-AMINO-5-(3-METHOXYPHENYL)-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL]BENZYL}PIPERIDIN-4-OL, Proto-oncogene tyrosine-protein kinase Src | Authors: | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | Deposit date: | 2005-01-27 | Release date: | 2006-01-27 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Crystal structures of active SRC kinase domain complexes J.Mol.Biol., 353, 2005
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1YOM
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![BU of 1yom by Molmil](/molmil-images/mine/1yom) | Crystal structure of Src kinase domain in complex with Purvalanol A | Descriptor: | 2-({6-[(3-CHLOROPHENYL)AMINO]-9-ISOPROPYL-9H-PURIN-2-YL}AMINO)-3-METHYLBUTAN-1-OL, Proto-oncogene tyrosine-protein kinase Src | Authors: | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | Deposit date: | 2005-01-27 | Release date: | 2006-01-27 | Last modified: | 2024-05-29 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Crystal structures of active SRC kinase domain complexes J.Mol.Biol., 353, 2005
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1YI6
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![BU of 1yi6 by Molmil](/molmil-images/mine/1yi6) | |
1Y6A
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![BU of 1y6a by Molmil](/molmil-images/mine/1y6a) | Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor | Descriptor: | N-[5-(ETHYLSULFONYL)-2-METHOXYPHENYL]-5-[3-(2-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-AMINE, Vascular endothelial growth factor receptor 2 | Authors: | Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A. | Deposit date: | 2004-12-05 | Release date: | 2005-06-07 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J.Med.Chem., 48, 2005
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1YOJ
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![BU of 1yoj by Molmil](/molmil-images/mine/1yoj) | Crystal structure of Src kinase domain | Descriptor: | proto-oncogene tyrosine-protein kinase SRC | Authors: | Breitenlechner, C.B, Kairies, N.A, Honold, K, Scheiblich, S, Koll, H, Greiter, E, Koch, S, Schaefer, W, Huber, R, Engh, R.A. | Deposit date: | 2005-01-27 | Release date: | 2006-01-27 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Crystal structures of active SRC kinase domain complexes J.Mol.Biol., 353, 2005
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1Y6B
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![BU of 1y6b by Molmil](/molmil-images/mine/1y6b) | Crystal structure of VEGFR2 in complex with a 2-anilino-5-aryl-oxazole inhibitor | Descriptor: | N-(CYCLOPROPYLMETHYL)-4-(METHYLOXY)-3-({5-[3-(3-PYRIDINYL)PHENYL]-1,3-OXAZOL-2-YL}AMINO)BENZENESULFONAMIDE, Vascular endothelial growth factor receptor 2 | Authors: | Harris, P.A, Cheung, M, Hunter, R.N, Brown, M.L, Veal, J.M, Nolte, R.T, Wang, L, Liu, W, Crosby, R.M, Johnson, J.H, Epperly, A.H, Kumar, R, Luttrell, D.K, Stafford, J.A. | Deposit date: | 2004-12-05 | Release date: | 2005-06-07 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J.Med.Chem., 48, 2005
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1YWN
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![BU of 1ywn by Molmil](/molmil-images/mine/1ywn) | Vegfr2 in complex with a novel 4-amino-furo[2,3-d]pyrimidine | Descriptor: | N-{4-[4-AMINO-6-(4-METHOXYPHENYL)FURO[2,3-D]PYRIMIDIN-5-YL]PHENYL}-N'-[2-FLUORO-5-(TRIFLUOROMETHYL)PHENYL]UREA, Vascular endothelial growth factor receptor 2 | Authors: | Miyazaki, Y, Matsunaga, S, Tang, J, Maeda, Y, Nakano, M, Philippe, R.J, Shibahara, M, Liu, W, Sato, H, Wang, L, Nolte, R.T. | Deposit date: | 2005-02-18 | Release date: | 2005-08-23 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.71 Å) | Cite: | Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors Bioorg.Med.Chem.Lett., 15, 2005
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