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.
Ki16425是竞争性的可逆的LPA拮抗剂,对LPA1,LPA2和LPA3的Ki分别为0.34 μM,6.5 μM和0.93 μM,而对LPA4,LPA5和LPA6无活性。
MoreMdivi-1是一个具有选择性和细胞穿膜性的线粒体分裂抑制剂,抑制DRP1(发动蛋白相关GTP酶)和Dynamin I (Dnm1)的IC50为1-10 μM。
MoreLY411575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。
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