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.
AZD2932是VEGFR-2和PDGFR的有效抑制剂,对PDGFRβ)、VEGFR-2和Flt-3的IC50值分别为4 nM、8 nM和7 nM。
MoreEPZ015666 是一种有效的,选择性且口服生物有效的 PRMT5 抑制剂,Ki 为 5 nM,选择性比其它 PMTs 高 20,000多倍。
MoreAndrographolide是一个不可逆的NF-κB通路拮抗剂,能阻止T细胞体外活化,抗病毒,抗炎,抗凋亡,降脂性能。
MoreAZD2858一种选择性的GSK-3抑制剂,IC50为68 nM,激活Wnt信号通路,增强大鼠的骨质。
More4SC-202 游离碱是特异的I型HDAC口服活性抑制剂(HDAC8除外),对HDAC1、2和3的IC50分别为1.2、1.12和0.57 uM,对IIa/IIb/III型HDAC的抑制性较弱。
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