Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21

Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21 Descriptor: (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-[(4-{[(2S)-2-(furan-2-yl)-2-hydroxyacetyl]amino}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide, G protein-coupled receptor kinase 5 Authors: Chen, Y, Tesmer, J.J.G. Deposit date: 2023-09-21 Release date: 2023-12-13 Last modified: 2024-10-23 Method: X-RAY DIFFRACTION (2.8 Å) Cite: Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes. Eur.J.Med.Chem., 264, 2023人源G蛋白偶联受体激酶5（G protein-coupled receptor kinase 5）与GRL018-21的复合物晶体结构 配体描述：(3Z)-N-[(1R)-1-(4-氟苯基)乙基]-3-[(4-{[(2S)-2-(呋喃-2-基)-2-羟基乙酰基]氨基}-3,5-二甲基-1H-吡咯-2-基)亚甲基]-2-氧代-2,3-二氢-1H-吲哚-5-甲酰胺 作者：Chen, Y、Tesmer, J.J.G. 提交日期：2023-09-21 发布日期：2023-12-13 最后修改日期：2024-10-23 实验方法：X射线衍射（X-RAY DIFFRACTION，分辨率2.8 Å） 引用文献：《一类新型强效高选择性G蛋白偶联受体激酶5抑制剂的开发及其抑制剂复合物晶体结构的结构洞察》，Eur.J.Med.Chem., 264, 2023