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.
EPZ-6438是一种有效的,选择性EZH2抑制剂,Ki为2.5 nM,比作用于EZH1选择性高35倍,比作用于14种其他HMT选择性高4500多倍。
MoreDoxycycline Hyclate是合成的四环素衍生物,有抗菌活性。
MoreMK-2206双盐酸盐是 Akt1/2/3的高选择性抑制剂,IC50分别为8 nM,12 nM和65 nM。
MoreS3I-201是一种STAT3选择性抑制剂,能够抑制STAT3-DNA结合活性,IC50为20 μM,对STAT1和STAT5抑制作用弱。
MoreGeldanamycin是HSP90抑制剂,Kd为1.2 μM。
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