Benzophenanthridinone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: Benzophenanthridinone
• 英文别名: 2H-benzo[k]phenanthridin-1-one
• 化学式: C₁₇H₁₁NO
• 分子量: 245.27
• InChiKey: XIUUWMMLYLBRBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  30
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] INHIBITORS OF KIDNEY-TYPE GLUTAMINASE, GLS-1<br/>[FR] INHIBITEURS DE LA GLUTAMINASE DE TYPE RÉNAL, GLS-1
  申请人：UNIV CORNELL

  公开号：WO2016090350A1

  公开（公告）日：2016-06-09

  The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

  本发明一般涉及具有式I、式II或式III的谷氨酸酶抑制剂，以及含有它们的药物化合物和它们的使用方法。
• Inhibitors of kidney-type glutaminase, GLS-1
  申请人：CORNELL UNIVERSITY

  公开号：US10889585B2

  公开（公告）日：2021-01-12

  The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

  本发明一般涉及式 I、式 II 或式 III 的谷氨酰胺酶抑制剂，以及含有它们的药物复合物和它们的使用方法。
• Labeled glutaminase proteins, isolated glutaminase protein mutants, methods of use, and kit
  申请人：CORNELL UNIVERSITY

  公开号：US11046945B2

  公开（公告）日：2021-06-29

  The present invention relates to a labeled glutaminase (GLS) protein comprising a GLS protein and a fluorescent reporter group attached to the GLS protein, wherein the fluorescent reporter group is attached to the GLS protein within the glutaminase domain pfam04960 of GLS. The present invention also relates to isolated glutaminase protein mutants. Also disclosed is a method of screening for compounds that allosterically bind to a glutaminase protein. The present invention also relates to a method of identifying compounds that inhibit or stabilize tetramer formation of glutaminase protein. The present invention further relates to a screening kit for compounds that inhibit or stabilize tetramer formation.

  本发明涉及一种标记的谷氨酰胺酶（GLS）蛋白，包括GLS蛋白和连接到GLS蛋白上的荧光报告基团，其中荧光报告基团在GLS的谷氨酰胺酶结构域pfam04960内连接到GLS蛋白上。本发明还涉及分离的谷氨酰胺酶蛋白突变体。本发明还公开了一种筛选与谷氨酰胺酶蛋白异构结合的化合物的方法。本发明还涉及一种鉴定抑制或稳定谷氨酰胺酶蛋白四聚体形成的化合物的方法。本发明还涉及一种筛选抑制或稳定四聚体形成的化合物的试剂盒。
• OXYNITIDINE DERIVATIVES USEFUL AS INHIBITORS OF TOPOISOMERASE IB (TOP1) AND/OR TYROSYL-DNA PHOSPHODIESTERASE 1 (TDP1)
  申请人：The United States of America, as represented by The Secretary, Department of Health and Human Services

  公开号：EP3826717A2

  公开（公告）日：2021-06-02
• LABELED GLUTAMINASE PROTEINS, ISOLATED GLUTAMINASE PROTEIN MUTANTS, METHODS OF USE, AND KIT
  申请人：CORNELL UNIVERSITY

  公开号：US20160002619A1

  公开（公告）日：2016-01-07

  The present invention relates to a labeled glutaminase (GLS) protein comprising a GLS protein and a fluorescent reporter group attached to the GLS protein, wherein the fluorescent reporter group is attached to the GLS protein within the glutaminase domain pfam04960 of GLS. The present invention also relates to isolated glutaminase protein mutants. Also disclosed is a method of screening for compounds that allosterically bind to a glutaminase protein. The present invention also relates to a method of identifying compounds that inhibit or stabilize tetramer formation of glutaminase protein. The present invention further relates to a screening kit for compounds that inhibit or stabilize tetramer formation.