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.
GM6001 (galardin, ilomastat)是泛MMP抑制剂,对MMP-1,MMP-2,MMP-3,MMP-7,MMP-8,MMP-9,MMP-12,MMP-14和MMP-26的Ki为0.4-27 nM。
MoreEPZ-005687是EZH2选择性抑制剂,Ki为24 nM,比作用于EZH1选择性高50倍,对其它15种甲基转移酶有500倍的选择性。
MoreNU7441 (KU-57788)是一种高度有效的,选择性DNA-PK抑制剂,IC50为14 nM,也能抑制PI3K,IC50为5 μM。
MoreJNK inhibitor IX 是一种高度选择性JNK抑制剂,其作用于JNK2和JNK3的pIC50分别为6.5和6.7。
MoreTriciribine是一种DNA合成抑制剂,也抑制Akt和HIV-1,IC50分别为130 nM和20 nM;对PI3K/PDK1没有抑制作用;作用于缺乏腺苷激酶的细胞,活性降低5000倍。
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