IRAK4-IN-13

• 常用名: IRAK4-IN-13
• 英文名: IRAK4-IN-13
• CAS号: 2667681-57-2
• 分子量: 457.53
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₇N₉O
• 熔点: N/A
• 闪点: N/A

IRAK4-IN-13用途

IRAK4-IN-13(化合物21)是一种有效和选择性IRAK4抑制剂,IC50为0.6 nM。IRAK4-IN-13显示出与人肝微粒体(HLM)的高代谢清除率。固有清除率为96µL/min/mg【1】。

IRAK4-IN-13名称

• 英文名: IRAK4-IN-13

IRAK4-IN-13生物活性

• 描述: IRAK4-IN-13(化合物21)是一种有效和选择性IRAK4抑制剂,IC50为0.6 nM。IRAK4-IN-13显示出与人肝微粒体(HLM)的高代谢清除率。固有清除率为96µL/min/mg【1】。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 免疫及炎症 >> IRAK
  信号通路 >> 蛋白酪氨酸激酶 >> IRAK
• 靶点实验:

  IRAK4:0.6 nM (IC50)

• 体外研究: IRAK4-IN-13(化合物21)显示细胞pIRAK4的效价,IC50为0.024µM【1】。IRAK4-IN-13(化合物21)显示出对IRAK4、IRAK1、BTK、Flt3、PI3Kδ、TRKa、TRKb、TRKc的选择性,IC50s分别为0.0006、0.002、0.044、1.2、0.018、0.019、0.082、0.036µM。
• 参考文献:

  [1]. Degorce SL, et al. Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors. Bioorg Med Chem. 2020 Dec 1;28(23):115815.

IRAK4-IN-13物理化学性质

• 分子式: C₂₄H₂₇N₉O
• 分子量: 457.53

IRAK4-IN-13靶点实验

查看更多实验

实验名称：Metabolic stability in human cytosol assessed as intrinsic clearance 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246644

实验名称：Metabolic stability in human hepatocytes assessed as intrinsic clearance measured per... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246641

实验名称：Metabolic stability in human liver microsomes assessed as intrinsic clearance 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246640

实验名称：Inhibition of IRAK4 (unknown origin) in presence of ATP by enzymatic assay 来源：ChEMBL 靶标：Interleukin-1 receptor-associated kinase 4 External Id：CHEMBL5246637

实验名称：Lipophilicity, LogD at pH 7.4 of the compound by shake flask method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246639

实验名称：Inhibition of IRAK4 (unknown origin) phosphorylation by cell based assay 来源：ChEMBL 靶标：Interleukin-1 receptor-associated kinase 4 External Id：CHEMBL5246638

实验名称：Selectivity index, ratio of IC50 for inhibition of TRKA (unknown origin) to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246689

实验名称：Selectivity index, ratio of IC50 for inhibition of PI3Kdelta (unknown origin) to IC50... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246688

实验名称：Selectivity index, ratio of IC50 for inhibition of TRKC (unknown origin) to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246691

实验名称：Selectivity index, ratio of IC50 for inhibition of TRKB (unknown origin) to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5246690

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