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.
GW9662是一种选择性PPAR拮抗剂,作用于PPARγ,IC50为3.3 nM,作用于PPARγ比作用于PPARα和PPARδ选择性强100到1000倍。
MoreScriptaid是HDAC抑制剂,相对于H3对乙酰化的H4效果更明显。
MoreMelatonin是由松果体产生的激素。
MoreGalunisertib是有效的TGFβ receptor I (TβRI)抑制剂,IC50为56 nM。
MoreRegorafenib (瑞格非尼; BAY 73-4506) 是多靶点抑制剂,对VEGFR1,VEGFR2,VEGFR3,PDGFRβ,Kit,RET和Raf-1的IC50分别为13 nM,4.2 nM,46 nM,22 nM,7 nM,1.5 nM和2.5 nM。
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