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.
Trilostane (曲洛司坦; Win 24540; Modrastane) 是3 β-羟化类固醇脱氢酶抑制剂,可作用于库兴氏综合症。
MoreCH5138303 是一种口服有效的Hsp90抑制剂,其Kd为 0.48 nM。
MoreTorcetrapib(CP-529414)是CETP高效抑制剂,IC50值为37nM。
MoreCNX-774是口服活性的高效Btk抑制剂,IC50< 1 nM,能与活性位点上的Cys-481形成配体导向的共价键。
MoreIndirubin是一具有抗炎症和抗癌活性的天然化合物。
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