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6MO9

N-terminal bromodomain of human BRD2 in complex with N-cyclopentyl-7-(3,5-dimethylisoxazol-4-yl)quinoline-5-sulfonamide inhibitor

6MO9 の概要
エントリーDOI10.2210/pdb6mo9/pdb
分子名称Bromodomain-containing protein 2, N-cyclopentyl-7-(3,5-dimethyl-1,2-oxazol-4-yl)quinoline-5-sulfonamide (3 entities in total)
機能のキーワードinhibitor, epigenetic reader, bromo domain, transcription-transcription inhibitor complex, transcription/transcription inhibitor
由来する生物種Homo sapiens (Human)
タンパク質・核酸の鎖数3
化学式量合計45863.67
構造登録者
Lansdon, E.B.,Newby, Z.E.R. (登録日: 2018-10-04, 公開日: 2019-01-23, 最終更新日: 2024-03-13)
主引用文献Sperandio, D.,Aktoudianakis, V.,Babaoglu, K.,Chen, X.,Elbel, K.,Chin, G.,Corkey, B.,Du, J.,Jiang, B.,Kobayashi, T.,Mackman, R.,Martinez, R.,Yang, H.,Zablocki, J.,Kusam, S.,Jordan, K.,Webb, H.,Bates, J.G.,Lad, L.,Mish, M.,Niedziela-Majka, A.,Metobo, S.,Sapre, A.,Hung, M.,Jin, D.,Fung, W.,Kan, E.,Eisenberg, G.,Larson, N.,Newby, Z.E.R.,Lansdon, E.,Tay, C.,Neve, R.M.,Shevick, S.L.,Breckenridge, D.G.
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Bioorg. Med. Chem., 27:457-469, 2019
Cited by
PubMed: 30606676
DOI: 10.1016/j.bmc.2018.11.020
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (1.801 Å)
構造検証レポート
Validation report summary of 6mo9
検証レポート(詳細版)ダウンロードをダウンロード

217705

件を2024-03-27に公開中

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