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.
Fasudil (HA-1077) HCl是一种有效的ROCK-II, PKA, PKG, PKC,和MLCK抑制剂, Ki分别为0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM,和36 μM。
MoreGefitinib (ZD1839)是一种EGFR酪氨酸激酶和Akt磷酸化抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173, Tyr992, Tyr1173和Tyr992时,IC50分别为37 nM, 37nM, 26 nM和57 nM。
MoreLDN-193189是一种选择性的BMP信号通路抑制剂,抑制BMP I型受体ALK2和ALK3的转录活性,IC50分别为5 nM和30 nM,作用于BMP比作用于TGF-β选择性高200倍。
MoreMGCD0103 (Mocetinostat)是HDAC抑制剂,对HDAC 1,HDAC 2和HDAC 3的IC50分别为0.15,0.29和1.66 μM。
MoreTeicoplanin是一种预防用的抗生素。
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