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.
Semagacestat是一种γ-分泌酶抑制剂,作用于Aβ42, Aβ40和Aβ38时,IC50分别为10.9 nM, 12.1 nM和12.0 nM,也抑制Notch信号通路,IC50为14.1 nM。
MoreBikinin(Abrasin)是植物GSK-3/Shaggy-like kinase高效抑制剂,活化油菜素内酯(BR)受体的下游信号。
MoreTAK-700 (Orteronel)是一种有效的,高度选择性的,人17,20-lyase抑制剂,IC50为38 nM,比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。Phase 3。
MoreUM729是一种新型的嘧啶吲哚,对AhR拮抗剂有协同效应,能抑制AML细胞的分化。
MoreOdanacatib (MK-0822)是一种有效的,选择性的,cathepsin K(人/兔)中性抑制剂,IC50为0.2 nM/1 nM,对脱靶的cathepsin B, L, S具有高度选择性。
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