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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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    VX-765 is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM.

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  • MK-8776 EY1525

    MK-8776 (SCH 900776)是一种选择性Chk1抑制剂，IC50为3 nM，比作用于Chk2选择性高50倍,是高效口服生物相容性的Chk1抑制剂,对Chk2和CDK2的IC50则分别为1500 nM和160 nM。

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  • C646 EY1542

    C646是一种histone acetyltransferase（组蛋白乙酰转移酶）抑制剂，抑制p300，Ki为400 nM，比作用于其他乙酰转移酶选择性高。

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  • Abiraterone EY1507

    Abiraterone是一种有效的类固醇细胞色素P450 17alpha-羟化酶-17， 20-裂解酶(CYP17)抑制剂，IC50为2 nM;对前列腺癌有活性。

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  • IM-12 EY1508

    IM-12是一种选择性的GSK-3β有效抑制剂，其IC50为53 nM。相比SB-216763，活性相当甚至要更好。

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