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.
A-966492是一种新型有效的PARP1和PARP2抑制剂,Ki分别为1 nM和1.5 nM。
MoreAZD8330是一种新型,选择性的,非ATP竞争性MEK 1/2抑制剂,IC50为7 nM。
MoreNVP-HSP990是Hsp90抑制剂,对Hsp90α的IC50值为13nM,抗癌增殖活性。
MoreGSK-J1是一个高效和选择性的H3K27去甲基化酶抑制剂,体外对人源JMJD3的IC50值为60 nM。
MoreChlorpheniramine是组胺H1受体拮抗剂,IC50为12 nM。
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