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.
Ketoconazole (酮康唑)是咪唑类抗真菌剂,是经典的CYP3A4抑制剂。
MoreMC1568是 class II (IIa)HDAC选择性抑制剂,对HDAC II的IC50值220nM,对class I HDAC活性弱176倍。
MorePD318088是ATP非竞争性MEK1/2变构抑制剂,能与ATP同时结合于MEK1,且其结合位点与ATP结合位点相邻。
MoreTenofovir Disoproxil FumarateDisoproxil Fumarate能阻断HIV-1和HBV的逆转录酶,对HIV-1和HIV-2的IC50分别为0.5-2.2 uM和1.6-4.9 uM。
MoreDanoprevir是HCV NS3/4A蛋白酶拟肽类抑制剂,IC50为0.2-3.5 nM,对HCV 1A/1B/4/5/6亚型的抑制性比对2B/3A亚型高10倍。
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