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.
GDC-0623是一种有效的 ATP 非竞争性MEK1抑制剂,Ki为 0.13 nM。
MoreCCT128930是ATP竞争性Akt2抑制剂,IC50为6 nM,比对其它PKA相关激酶的抑制性强28倍以上。
MoreMitiglinide Calcium是KATP通道拮抗剂,具有抗2型糖尿病活性。
MoreMizolastine是组胺H1受体拮抗剂,IC50为47 nM。
MoreTasquinimod(ABR-215050)是喹啉-3-甲酰胺利诺胺类似物,具有抗血管生成和抗肿瘤活性。
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