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.
Ubenimex (Bestatin)是一种竞争性氨肽酶B抑制剂,作用于K562细胞,IC50为100 mg/ml。
MoreNilotinib (尼洛替尼; AMN-107) 是Bcr-Abl抑制剂,IC50小于30 nM。
MoreSB431542是一种有效的,选择性的ALK5抑制剂,IC50为94 nM,对ALK5的作用比对p38,MAPK和其他激酶强100倍。
MoreJIB-04是一个对Jumonji组蛋白脱甲基酶选择性的广谱抑制剂,对JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C和JMJD2D的IC50分别是230 nM、340 nM、855 nM、445 nM、435 nM、1100 nM和290 nM。
MoreLamivudine (拉米夫定) 为核苷类似物,是逆转录酶抑制剂,IC50为2.7 mM。
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