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.
Immethridine dihydrobromide是活性的 H3 激动剂(highly selective over H4)。
MoreBMS-626529是HIV-1 gp120抑制剂,能阻止其与CD4+ T细胞的结合。
MoreSunitinib Malate是一种多靶点受体酪氨酸激酶(RTK)抑制剂,作用于VEGFR1, VEGFR2, VEGFR3, PDGFRβ, FLT3,和CSF-1R时,IC50分别为15 nM, 38 nM, 30 nM, 55 nM, 21 nM,和35 nM。
MoreErlotinib HCl (OSI-744)是一种EGFR抑制剂,IC50为2 nM,对EGFR的选择性比c-Src或v-Abl高1000倍以上。
MoreSorafenib Tosylate是酪氨酸激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂,同时作用于Raf-1,wtBRAF和V599EBRAF,IC50分别为6 nM, 22 nM和38 nM。
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