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.
MK-801 (Dizocilpine)是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂,Ki为30.5 nM。
MoreAZD1208是口服活性的PIM高选择性抑制剂,对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。
MorePD153035 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。
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