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.
PD153035 Hcl (ZM 252868; AG 1517)是高活性EGFR选择性抑制剂,Ki和IC50分别为5.2 pM和29 pM,而对PGDFR,FGFR,CSF-1,InsR和Src活性极低。
MoreSSR128129E是FGFR激酶家族变构阻断剂,能结合FGFR胞外结构域并阻断FGFR的信号转导。
MoreNaloxone盐酸盐是阿片类拮抗剂,对阿片受体的IC50为3 nM。
MoreGW0742是一种有效的,选择性PPARβ/δ激动剂,IC50为1 nM,比作用于hPPARα和hPPARγ选择性高1000倍。
MoreBatimastat (BB-94)是一种广谱MMP(基质金属蛋白酶)抑制剂,作用于MMP-1, MMP-2, MMP-9, MMP-7和MMP-3,IC50分别为3 nM, 4 nM, 4 nM, 6 nM和20 nM。
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