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.
EI1是EZH2选择性抑制剂,对野生型EZH2和EZH2 Y641F突变型的IC50分别为15 nM和13 nM。
MoreOzagrel是高选择性的血栓素a2(TXA2)合成酶抑制剂。
MoreAdefovir Dipivoxil可阻断HBV逆转录酶。
MoreBMN 673是一种新型的PARP抑制剂,IC50为0.58 nM,也有效抑制PARP-2,但不抑制PARG,对PTEN突变型高度敏感。
MoreSNX-2112选择性结合到HSP90α和HSP90β的ATP结合袋中,Ka分别为30 nM和30 nM,比17-AAG更有效。
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