CCG-273463

• 常用名: CCG-273463
• 英文名: CCG-273463
• CAS号: 2750413-99-9
• 分子量: 521.41
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₆H₂₅BrN₄O₃
• 熔点: N/A
• 闪点: N/A

CCG-273463用途

CCG-273463是一种有效、选择性和共价的GRK5抑制剂,IC50值为9 nM。CCG-273463可用于心力衰竭、肥厚性心肌病和癌症的研究[1]。

CCG-273463名称

• 英文名: CCG-273463

CCG-273463生物活性

• 描述: CCG-273463是一种有效、选择性和共价的GRK5抑制剂,IC50值为9 nM。CCG-273463可用于心力衰竭、肥厚性心肌病和癌症的研究[1]。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 心血管疾病
• 靶点实验:

  IC50: 8.6 nM (GRK5), 12 μM (GRK2)[1].

• 体外研究: CCG-273463(0.02-1μM)有效且高度抑制GRK5(IC50:9 nM),在1μM时抑制率为93%(GRK5)和97%(GRK6)[1]。
• 参考文献:

  [1]. Rachel A Rowlands, et al. Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem. 2021 Jan 14;64(1):566-585.

CCG-273463物理化学性质

• 分子式: C₂₆H₂₅BrN₄O₃
• 分子量: 521.41

CCG-273463靶点实验

查看更多实验

实验名称：Inhibition of human GRK5 using porcine brain tubulin as substrate incubated for 3 to ... 来源：ChEMBL 靶标：G protein-coupled receptor kinase 5 External Id：CHEMBL4775842

实验名称：Inhibition of GRK3 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Beta-adrenergic receptor kinase 2 External Id：CHEMBL4775843

实验名称：Inhibition of bovine GRK2 using porcine brain tubulin as substrate incubated for 3 to... 来源：ChEMBL 靶标：Beta-adrenergic receptor kinase 1 External Id：CHEMBL4775830

实验名称：Selectivity index, ratio of IC50 for bovine GRK2 to IC50 for human GRK5 using porcine... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4775831

实验名称：Inhibition of GRK6 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：G protein-coupled receptor kinase 6 External Id：CHEMBL4775844

实验名称：Inhibition of human GRK5 using porcine brain tubulin as substrate incubated for 3 to ... 来源：ChEMBL 靶标：G protein-coupled receptor kinase 5 External Id：CHEMBL4775829

实验名称：Inhibition of PKA (unknown origin) incubated for 30 mins using REBtide substrate by A... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4775845

实验名称：Covalent binding affinity to GRK5 (unknown origin) assessed as covalent adduct format... 来源：ChEMBL 靶标：G protein-coupled receptor kinase 5 External Id：CHEMBL4775834

实验名称：Selectivity index, ratio of IC50 for human GRK5 C474S mutant to IC50 for human GRK5 u... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4775838

实验名称：Covalent inhibition of GRK5 (unknown origin) using porcine brain tubulin as substrate... 来源：ChEMBL 靶标：G protein-coupled receptor kinase 5 External Id：CHEMBL4775836

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