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.
IM-12是一种选择性的GSK-3β有效抑制剂,其IC50为53 nM。相比SB-216763,活性相当甚至要更好。
MoreGM6001 (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。
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