タイトル | Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors. |
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ジャーナル・号・ページ | J. Am. Chem. Soc., Vol. 131, Page 13286-13296, Year 2009 |
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掲載日 | 2009年2月22日 (構造データの登録日) |
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著者 | Simard, J.R. / Getlik, M. / Grutter, C. / Pawar, V. / Wulfert, S. / Rabiller, M. / Rauh, D. |
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リンク | J. Am. Chem. Soc. / PubMed:19572644 |
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手法 | X線回折 |
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解像度 | 2 - 2.3 Å |
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構造データ | PDB-3gcp: Human P38 MAP Kinase in Complex with SB203580 手法: X-RAY DIFFRACTION / 解像度: 2.25 Å PDB-3gcq: Human P38 MAP kinase in complex with RL45 手法: X-RAY DIFFRACTION / 解像度: 2.0 Å PDB-3gcs: Human P38 MAP kinase in complex with Sorafenib 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-3gcu: Human P38 MAP kinase in complex with RL48 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-3gcv: Human P38 MAP Kinase in Complex with RL62 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å |
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化合物 | ChemComp-SB2: 4-[5-(4-FLUORO-PHENYL)-2-(4-METHANESULFINYL-PHENYL)-3H-IMIDAZOL-4-YL]-PYRIDINE
ChemComp-1BU: 1-{4-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea
ChemComp-BAX: 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE / ソラフェニブ / 阻害剤*YM
ChemComp-R48: 1-{3-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]urea
ChemComp-SS6: 1-{3-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea
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由来 | homo sapiens (ヒト)
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キーワード | TRANSFERASE / DFG-out / Type I / SB203580 / Alternative splicing / ATP-binding / Cytoplasm / Kinase / Nucleotide-binding / Nucleus / Phosphoprotein / Polymorphism / Serine/threonine-protein kinase / Type II / BAY439006 |
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