4-((5-((4-(3-氯苯基)-3-氧代哌嗪-1-基)甲基)-1H-咪唑-1-基)甲基)苯甲腈

• 常用名: 4-((5-((4-(3-氯苯基)-3-氧代哌嗪-1-基)甲基)-1H-咪唑-1-基)甲基)苯甲腈
• 英文名: L-778,123
• CAS号: 183499-57-2
• 分子量: 405.88
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₂₀ClN₅O
• 熔点: N/A
• 闪点: N/A

用途

L-778123是FPTase和GGPTase-I双重抑制剂, IC50值分别为2 nM 和 98 nM。

名称

• 中文名: 4-((5-((4-(3-氯苯基)-3-氧代哌嗪-1-基)甲基)-1H-咪唑-1-基)甲基)苯甲腈
• 英文名: 1-(3-chlorophenyl)-4-[1-(4-cyanobenzyl)-5-imidazolyl methyl]-2-piperazinone

生物活性

• 描述: L-778123是FPTase和GGPTase-I双重抑制剂, IC50值分别为2 nM 和 98 nM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> 法呢基转移酶
• 参考文献:

  [1]. Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758.

  [2]. Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77.

物理化学性质

• 分子式: C₂₂H₂₀ClN₅O
• 分子量: 405.88
• 精确质量: 405.13600
• PSA: 65.16000
• LogP: 3.30818
• InChIKey: JNUGFGAVPBYSHF-UHFFFAOYSA-N
• SMILES: N#Cc1ccc(Cn2cncc2CN2CCN(c3cccc(Cl)c3)C(=O)C2)cc1
• 储存条件: 室温，干燥密封

靶点实验

查看更多实验

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实验名称：Inhibition of Farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinan... 来源：ChEMBL 靶标：Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha External Id：CHEMBL681407

实验名称：Partition coefficient (logP) 来源：ChEMBL 靶标：N/A External Id：CHEMBL630187

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry 来源：NCGC 靶标：N/A External Id：TRND-SARS-CoV-2-cytotox-48hr

实验名称：Inhibition of Farnesyltransferase 来源：ChEMBL 靶标：Protein farnesyltransferase subunit beta External Id：CHEMBL682065

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实验名称：Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat... 来源：ChEMBL 靶标：Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha External Id：CHEMBL685969

实验名称：Reactivation of latent HIV-1 infected in human Jurkat 2C4 cells assessed as increase ... 来源：ChEMBL 靶标：Human immunodeficiency virus 1 External Id：CHEMBL4724690

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英文别名

• 4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile
• 4-[(5-{[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl}-1H-imidazol-1-yl)methyl]benzonitrile
• 1-(3-chlorophenyl)-4-[1-(4-cyanobenzyl)-5-imidazolyl-methyl]-2-piperazinone
• 1-(3-Chlorophenyl)-4-[1-(4-cyanobenzyl)-5-imidazolylmethyl]-2-piperazinone
• 1-(3-chlorophenyl)-4-[1-(4-cyanobenzyl)imidazolyl-methyl]-2-piperazinone
• L-778123