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.
CEP-33779是JAK2新型选择性高效抑制剂,IC50值为1.8nM。
MoreAZ 960是一种新型的,ATP竞争性的JAK2抑制剂,IC50和Ki分别低于3 nM和0.45 nM,作用于JAK2比作用于JAK3选择性高3倍。
MorePyrimethamine可通过抑制二氢叶酸还原酶(DHFR)干扰四氢叶酸的合成,可作用于原生动物的感染。
MoreRamelteon是褪黑激素受体MT1/2选择性激动剂,对MT1和MT2的IC50分别为28.5 pM和20.1 pM。
MoreLedipasvir是HCV NS5A抑制剂。
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