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.
JIB-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。
MoreGanetespib (STA-9090)是一种HSP90抑制剂,作用于OSA 8种细胞,IC50为4 nM,诱导OSA细胞凋亡,而对正常的成骨细胞无作用;是STA-1474的活性代谢物。
MoreSB-3CT是Gelatinase高效选择性抑制剂,对MMP2和MMP9的Ki值分别为13.9nM和600nM。
MoreFingolimod (FTY720) HCl是一种1-磷酸-神经鞘氨醇S1P受体拮抗剂,IC50为0.33 nM。
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