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.
PCI-24781是一种新型的pan-HDAC抑制剂,靶向作用于HDAC1,Ki为7 nM,对HDACs 2, 3, 6,和10有适中的抑制性,但比作用于HDAC8选择性强40倍。
MoreLY-2584702是p70S6K信号转导口服性抑制剂,能抑制和阻止核糖体S6亚基的磷酸化。
MoreMEK162(ARRY-438162; ARRY-162)是MEK1/2抑制剂,IC50为12 nM。
MoreTicagrelor是第一个结合可逆的口服P2Y12受体拮抗剂,Ki为2 nM,还能抑制CYP2C9,IC50为10.5 μM。
MoreMevastatin (Compactin; ML236B)抑制HMG-CoA还原酶(HMGCR),可抑制类异戊二烯的生物合成,阻断蛋白的异戊二烯化,降低血浆胆固醇水平。
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