6IAR

Tricyclic indazoles a novel class of selective estrogen receptor degrader antagonists

6IAR の概要

• エントリーDOI: 10.2210/pdb6iar/pdb
• 分子名称: Estrogen receptor, 3-[4-[(6~{R})-7-(2-methylpropyl)-3,6,8,9-tetrahydropyrazolo[4,3-f]isoquinolin-6-yl]phenyl]propanoic acid (3 entities in total)
• 機能のキーワード: nuclear hormone receptor inhibitor downregulation estrogen receptor modulators, dna binding protein
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 27470.29

構造登録者

Scott, J.S.,Bailey, A.,Buttar, D.,Carbajo, R.J.,Curwen, J.,Davies, R.D.M.,Degorce, S.L.,Donald, C.,Gangl, E.,Greenwood, R.,Groombridge, S.D.,Johnson, T.,Lamont, S.,Lawson, M.,Lister, A.,Morrow, C.,Moss, T.,Pink, J.H.,Polanski, R. (登録日: 2018-11-27, 公開日: 2019-01-23, 最終更新日: 2024-05-15)

• 主引用文献: Scott, J.S.,Bailey, A.,Buttar, D.,Carbajo, R.J.,Curwen, J.,Davey, P.R.J.,Davies, R.D.M.,Degorce, S.L.,Donald, C.,Gangl, E.,Greenwood, R.,Groombridge, S.D.,Johnson, T.,Lamont, S.,Lawson, M.,Lister, A.,Morrow, C.J.,Moss, T.A.,Pink, J.H.,Polanski, R.; Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.; J.Med.Chem., 62:1593-1608, 2019; PubMed: 30640465; DOI: 10.1021/acs.jmedchem.8b01837

実験手法

X-RAY DIFFRACTION (1.84 Å)