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.
Olaparib (AZD2281, Ku-0059436)是一种选择性的PARP1/2抑制剂,IC50为5 nM/1 nM,比对Tankyrase-1的抑制作用强300倍。
MoreSCH772984是一种新型特异性的ERK1/2抑制剂, IC50分别为4 Nm/1 nM。
MoreMycophenolic acid是一种免疫抑制剂,用于预防器官移植排斥。
MoreU-73122是磷脂酶C/A2和5-脂氧合酶(5-LO)抑制剂。
MoreCHIR-99021 (CT99021)是GSK-3α和β抑制剂,IC50分别为10 nM和6.7 nM,比对CDC2,ERK2及其他激酶的抑制性强500倍。
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