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.
Cerdulatinib (PRT-062070)是一种具有口服活性的多靶点酪氨酸激酶抑制剂,对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶,IC50均低于200 nM。
MoreLoperamide hydrochloride是阿片类受体激动剂,是长效止泻剂。
MoreCUDC-907是I型PI3K和I、II型HDA的双重C抑制剂,对PI3Kα/β/δ的IC50分别为19/54/39 nM,对HDAC1/2/3/10的IC50分别为1.7/5.0/1.8/2.8 nM。
MoreLimonin为柑橘类水果中富含的三萜类化合物,具有抗病毒和抗肿瘤活性。
MorePFI-2是甲基转移酶SETD7高效选择性抑制剂,IC50值为2nM。
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