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.
Givinostat (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。
MoreChloroquine Phosphate是一种4-氨基喹啉的抗疟疾和抗风湿抑制剂。
MoreLonafarnib(Sch66336)是口服生物相容性的FPTase抑制剂,对H-ras,K-ras-4B和N-ras的IC50分别为1.9 nM,5.2 nM和2.8 nM。
MoreEHop-016是Rac GTPase高效选择性抑制剂,在MDA-MB-435细胞中IC50值1.1uM。
MoreVeliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂,Ki分别为5.2 nM和2.9 nM,抑制SIRT2。
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