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.
LY411575是一种有效的γ-secretase抑制剂,IC50为0.078 nM/0.082 nM(基于膜/细胞),也抑制Notch分裂,IC50为0.39 nM。
MoreRKI-1447是ROCK1和ROCK2的抑制剂,IC50分别为15.4 nM和6.2 nM。
MoreUNC1999一种有效的具有口服活性的EZH1、EZH2选择性抑制剂,其IC50分别为2 nM和45 nM,对很多表观遗传学相关或不相关的靶点选择性大于1000倍。
MoreR428是Axl抑制剂,IC50为14 nM。
MoreLMK235 是HDAC 抑制剂,对HDAC4 和 HDAC5具有特异性抑制作用,IC50值为 0.49 μM (A2780)、 0.32 μM (A2780 CisR)。
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