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.
GW501516是高活性PPARβ/δ选择性激动剂,EC50为1 nM,比对hPPARα和hPPARγ的抑制性强1000倍。
MoreLatrepirdine是一种抗组织胺的药物。
MoreIspinesib是一种有效的,特异性的,可逆的kinesin spindle protein (KSP)(纺锤体驱动蛋白)抑制剂,Kiapp为1.7 nM,对CENP-E, RabK6, MCAK, MKLP1, KHC和Kif1A没有抑制作用。
MoreTeriflunomide是Leflunomide的活性代谢物,通过抑制酶二氢乳清酸脱氢酶,从而抑制嘧啶从头合成,作为一种免疫调节剂。
MoreSildenafil citrate是磷酸二酯酶5(PDE-5)抑制剂,IC50为5.22 nM,可能是最好的可作用于勃起功能紊乱的化合物。
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