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.
Tolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂,Ki为30nM。
MoreA-438079盐酸盐是P2X7受体拮抗剂,能抑制人重组P2X7细胞系的钙流,pIC50为6.9。
MoreZM39923盐酸盐是一种JAK1/3抑制剂, pIC50 of 4.4/7.1, 对JAK2几乎没有抑制活性。
MoreApremilast是一种口服生物有效的PDE4和TNF-α抑制剂,IC50分别为74 nM和77 nM。
MorePP-121是多靶点抑制剂,对于PDGFR,Hck,mTOR,VEGFR2,Src和Abl的IC50分别为2 nM,8 nM,10 nM,12 nM,14 nM和18 nM,同时还可抑制DNA-PK(IC50为60 nM)。
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