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.
A922500是人类和小鼠DGAT-1抑制剂,IC50分别为7 nM和24 nM,比作用于相关的酰基转移酶,hERG及抗靶面板的选择性高。
MoreDesonide是非氟化皮质类固醇抗炎剂,能作用于糖皮质激素受体。
MoreLY2090314是高活性GSK-3抑制剂,对GSK-3α和GSK-3β的IC50分别为1.5 nM和0.9 nM。可提高以铂类为基础的化疗方案的疗效。
MoreKU-0060648是DNA-PK和PI3Kα/β/δ双重抑制剂,IC50分别为8.6 nM和4 nM/0.5 nM/0.1 nM,对PI3Kγ抑制作用稍弱,IC50为0.59 μM。
MoreZalcitabine是一种核苷类HIV逆转录酶抑制剂(NARTI)。
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