EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
ジャーナル・号・ページ	Bioorg. Med. Chem. Lett., Vol. 21, Page 6188-6194, Year 2011
掲載日	2011年7月7日 (構造データの登録日)
著者	Liddle, J. / Atkinson, F.L. / Barker, M.D. / Carter, P.S. / Curtis, N.R. / Davis, R.P. / Douault, C. / Dickson, M.C. / Elwes, D. / Garton, N.S. ...Liddle, J. / Atkinson, F.L. / Barker, M.D. / Carter, P.S. / Curtis, N.R. / Davis, R.P. / Douault, C. / Dickson, M.C. / Elwes, D. / Garton, N.S. / Gray, M. / Hayhow, T.G. / Hobbs, C.I. / Jones, E. / Leach, S. / Leavens, K. / Lewis, H.D. / McCleary, S. / Neu, M. / Patel, V.K. / Preston, A.G. / Ramirez-Molina, C. / Shipley, T.J. / Skone, P.A. / Smithers, N. / Somers, D.O. / Walker, A.L. / Watson, R.J. / Weingarten, G.G.
リンク	Bioorg. Med. Chem. Lett. / PubMed:21903390
手法	X線回折
解像度	1.32 - 2.22 Å
構造データ	PDB-3srv: Crystal structure of spleen tyrosine kinase (SYK) in complex with a diaminopyrimidine carboxamide inhibitor 手法: X-RAY DIFFRACTION / 解像度: 1.95 Å PDB-4yjo: THE KINASE DOMAIN OF HUMAN SPLEEN TYROSINE (SYK) IN COMPLEX WITH GTC000222 手法: X-RAY DIFFRACTION / 解像度: 1.6 Å PDB-4yjp: THE KINASE DOMAIN OF HUMAN SPLEEN TYROSINE (SYK) IN COMPLEX WITH GTC000223 手法: X-RAY DIFFRACTION / 解像度: 1.83 Å PDB-4yjq: SYK kinase domain in complex with inhibitor GTC000224 手法: X-RAY DIFFRACTION / 解像度: 1.34 Å PDB-4yjr: SYK kinase domain in complex with inhibitor GTC000225 手法: X-RAY DIFFRACTION / 解像度: 1.32 Å PDB-4yjs: THE KINASE DOMAIN OF HUMAN SPLEEN TYROSINE (SYK) IN COMPLEX WITH GTC000226 手法: X-RAY DIFFRACTION / 解像度: 2.22 Å PDB-4yjt: THE KINASE DOMAIN OF HUMAN SPLEEN TYROSINE (SYK) IN COMPLEX WITH GTC000233 手法: X-RAY DIFFRACTION / 解像度: 1.52 Å PDB-4yju: THE KINASE DOMAIN OF HUMAN SPLEEN TYROSINE (SYK) IN COMPLEX WITH GTC000249 手法: X-RAY DIFFRACTION / 解像度: 1.67 Å
化合物	ChemComp-S19: 2-{[(3R,4R)-3-aminotetrahydro-2H-pyran-4-yl]amino}-4-[(4-methylphenyl)amino]pyrimidine-5-carboxamide ChemComp-GOL: GLYCEROL / グリセロ-ル / グリセリン ChemComp-HOH: WATER / 水 ChemComp-4DF: 5-chloro-N~2~-(1,1-dioxido-2,3-dihydro-1,2-benzothiazol-6-yl)-N~4~-ethyl-N~4~-(1H-indazol-4-yl)pyrimidine-2,4-diamine ChemComp-4DL: 2-[{2-[(1,1-dioxido-2,3-dihydro-1,2-benzothiazol-6-yl)amino]pyrimidin-4-yl}(1H-indazol-4-yl)amino]ethanol ChemComp-DMS: DIMETHYL SULFOXIDE / 2-チアプロパン2-オキシド / DMSO, 沈殿剤YM / ジメチルスルホキシド ChemComp-4DK: 3-[1H-indazol-4-yl(2-{[3-(4-methyl-1,3-oxazol-5-yl)phenyl]amino}pyrimidin-4-yl)amino]propan-1-ol ChemComp-4DJ: 3-(1H-indazol-4-yl{2-[(1-methyl-1H-indazol-5-yl)amino]pyrimidin-4-yl}amino)propan-1-ol ChemComp-4DN: 3-[{2-[(1,1-dioxido-2,3-dihydro-1,2-benzothiazol-6-yl)amino]pyrimidin-4-yl}(1H-indazol-4-yl)amino]propan-1-ol ChemComp-4DQ: N~2~-(1,1-dioxido-2,3-dihydro-1,2-benzothiazol-6-yl)-N~4~-ethyl-5-fluoro-N~4~-(1H-indazol-4-yl)pyrimidine-2,4-diamine ChemComp-4DO*: N~2~-(1,1-dioxido-2,3-dihydro-1,2-benzothiazol-6-yl)-5-fluoro-N~4~-(1H-indazol-4-yl)-N~4~-methylpyrimidine-2,4-diamine
由来	homo sapiens (ヒト)
キーワード	TRANSFERASE/TRANSFERASE INHIBITOR / SK363 / SYK / non-receptor tyrosine kinase / spleen tyrosine kinase / TRANSFERASE (転移酵素) / PHOSPHORYLATION (リン酸化) / TRANSFERASE-TRANSFERASE INHIBITOR complex