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.
NU7026是一种有效的DNA-PK抑制剂,IC50为0.23 μM,作用于DNA-PK比作用于PI3K选择性高60倍,抑制ATM和ATR活性。
MorePioglitazone hydrochloride (盐酸吡格列酮; U 72107A; AD 4833) 是PPARγ刺激剂。
MoreGSK690693是Akt1/2/3抑制剂,IC50分别为2 nM,13 nM和9 nM。同时还对PKA,PrkX和PKC同工酶有抑制性。
MoreOG-L002是一种有效的,特异性的LSD1抑制剂,IC50为20 nM,比作用于MAO-B和MAO-A选择性分别高36和69倍。
MoreTG-101348 (SAR302503)是JAK2选择性抑制剂,IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,同时还能抑制BRD4,IC50为340 nM。
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