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.
PH-797804是一种新型吡啶酮抑制剂,作用于p38α,IC50为26 nM;比作用于p38β选择性高4倍以上,不抑制JNK2。
MoreAUY922 (NVP-AUY922)是高活性HSP90α和β抑制剂,IC50为13 nM和21 nM,对GRP94和 TRAP-1的活性较低。
MoreRG2833(RGFP109)是可通过血脑屏障的HDAC抑制剂,对HDAC1和HDAC3的IC50分别为60nM和50nM。
MorePomalidomide能抑制LPS诱导的TNF-α释放,IC50为13 nM。
MorePD0325901是一种选择性的,ATP非竞争性的MEK抑制剂,IC50为0.33 nM,对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。
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