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Signal Pathway


In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.

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    NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50 小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。

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  • Dolutegravir EY1145

    Dolutegravir 是整合酶抑制剂，IC50为2.7 nM，对raltegravir-抗性的突变型Y143R，Q148K，N155H和G140S/Q148H有一定抑制性。

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  • LB42708 EY1148

    LB42708 是一种口服有效的 farnesyltransferase (FTase) 抑制剂。

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  • PF-4981517 EY1121

    PF-4981517是一种有效的，选择性的CYP3A4(P450)抑制剂，IC50为0.03 μM，比作用于CYP3A5和CYP3A7选择性高500倍以上。

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  • MK-8245 EY1125

    MK-8245是一种靶向作用于肝脏的stearoyl-CoA desaturase (SCD)（硬脂酰辅酶A去饱和酶）抑制剂，作用于人类SCD1时，IC50为1 nM，作用于大鼠和小鼠SCD1时，IC50为3 nM，具有抗糖尿病和抗高脂血症作用。

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