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.
Sorafenib 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。
MoreE-64 是一种作用于木瓜蛋白酶的选择性的不可逆的半胱氨酸蛋白酶抑制剂,其IC50为9 nM。
MoreYO-01027是一种二肽γ-secretase抑制剂,抑制APPL和Notch分裂, IC50分别为2.6 nM和2.9 nM。
MoreG418 (Geneticin)是氨基糖苷类抗生素,结构与庆大霉素B1相似,在原核和真核细胞中均能通过抑制延伸步骤来阻断多肽合成。
MoreGSK-LSD1 2HCl是一种不可逆的选择性 LSD1抑制剂,IC50 为 16 nM,选择性比其它密切相关的FAD可利用酶(即 LSD2,MAO-A,MAO-B)高1000多倍。
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