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.
SL-327是可渗透入细胞的MEK-1和MEK-2抑制剂,IC50分别为180nM和220nM。
MoreEtravirine是非核苷类逆转录酶抑制剂,对野生型HIV-1的EC50为1.4 nM到4.8 nM。
MoreAdapalene (阿达帕林; CD-271; Differin) 是合成的维甲酸,为维甲酸受体(RAR)激动剂。
MoreDarifenacin hydrobromide (氢溴酸达非那新; UK88525) 是选择性M3蕈毒碱受体拮抗剂,pKi为8.9。
MorePAC-1是首个Caspase活化化合物,EC50值为0.22uM,能增强procaspase-3活性并诱导多种癌细胞和小鼠肿瘤模型凋亡。
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