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 a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
ジャーナル・号・ページ	J. Med. Chem., Vol. 60, Page 695-709, Year 2017
掲載日	2016年12月5日 (構造データの登録日)
著者	Humphreys, P.G. / Bamborough, P. / Chung, C.W. / Craggs, P.D. / Gordon, L. / Grandi, P. / Hayhow, T.G. / Hussain, J. / Jones, K.L. / Lindon, M. ...Humphreys, P.G. / Bamborough, P. / Chung, C.W. / Craggs, P.D. / Gordon, L. / Grandi, P. / Hayhow, T.G. / Hussain, J. / Jones, K.L. / Lindon, M. / Michon, A.M. / Renaux, J.F. / Suckling, C.J. / Tough, D.F. / Prinjha, R.K.
リンク	J. Med. Chem. / PubMed:28002667
手法	X線回折
解像度	1.62 - 1.8 Å
構造データ	PDB-5mkx: 1.68A STRUCTURE PCAF BROMODOMAIN WITH 4-chloro-2-methyl-5-(methylamino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.68 Å PDB-5mky: BROMODOMAIN OF HUMAN BRD9 WITH 4-chloro-2-methyl-5-((2-methyl-1,2,3,4-tetrahydroisoquinolin-5-yl)amino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.67 Å PDB-5mkz: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 4-chloro-2-methyl-5-(((3-methylthiophen-2-yl)methyl)amino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.62 Å PDB-5ml0: Bromodomain of Mouse PCAF with (R)-4-chloro-2-methyl-5-((1-methylpiperidin-3-yl)amino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.64 Å PDB-5mli: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 4-chloro-2-methyl-5-(methylamino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.63 Å PDB-5mlj: Bromodomain of Human GCN5 with 4-bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one 手法: X-RAY DIFFRACTION / 解像度: 1.8 Å
化合物	ChemComp-82I: 4-chloranyl-2-methyl-5-(methylamino)pyridazin-3-one / 2-メチル-4-クロロ-5-(メチルアミノ)ピリダジン-3(2H)-オン ChemComp-SO4: SULFATE ION / 硫酸ジアニオン ChemComp-EPE: 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID / HEPES / pH緩衝剤YM ChemComp-BU1: 1,4-BUTANEDIOL / 1,4-ブタンジオ-ル ChemComp-HOH: WATER ChemComp-I0D: 4-chloranyl-2-methyl-5-[(2-methyl-3,4-dihydro-1~{H}-isoquinolin-5-yl)amino]pyridazin-3-one ChemComp-RNK: 4-chloranyl-2-methyl-5-[(3-methylthiophen-2-yl)methylamino]pyridazin-3-one ChemComp-GOL: GLYCEROL / グリセロ-ル ChemComp-P2L: 4-chlorol-2-methyl-5-[[(3~{R})-1-methylpiperidin-3-yl]amino]pyridazin-3-one ChemComp-EDO: 1,2-ETHANEDIOL / エチレングリコ-ル ChemComp-9ST*: 4-bromo-2-methyl-5-[[(3~{R},5~{R})-1-methyl-5-phenyl-piperidin-3-yl]amino]pyridazin-3-one / GSK-4027
由来	homo sapiens (ヒト) mus musculus (ハツカネズミ)
キーワード	TRANSCRIPTION / INHIBITOR / HISTONE / EPIGENETIC READER / BROMODOMAIN / PCAF / ANTAGONIST / BRD9 / BRD4 / BROMODOMAIN CONTAINING PROTEIN 4 / GCN5 / KAT2A