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.
Imatinib Mesylate (STI571)是Imatinib的甲磺酸盐,具有较好的口服生物利用度,是一种多靶点的抑制剂,同时作用于v-Abl, c-Kit和PDGFR,IC50分别为0.6 μM, 0.1 μM 和0.1 μM。
MoreImatinib (STI571)是一种多靶点酪氨酸激酶抑制剂,作用于v- v-Abl, c-Kit和PDGFR 时,IC50分别为0.6, 0.1和0.1 μM。
MoreDasatinib是一种Src/Abl抑制剂,IC50分别为0.6 nM和0.8 nM。
MoreJSH-23抑制NF-κB的转录活性,IC50为7.1 μM。
MoreGivinostat (ITF2357)是一种有效的HDAC抑制剂,作用于HDAC2, HDAC1B和HDAC1A时,IC50分别为10 nM, 7.5 nM和16 nM。
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