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.
MI-2 (Menin-MLL Inhibitor)是一种有效的menin-MLL相互作用抑制剂,IC50为446 nM。
MoreEmpagliflozin (BI 10773)是一种有效的,选择性SGLT-2抑制剂,IC50为3.1 nM,比作用于SGLT-1, 4, 5和6选择性高300倍以上。
MoreLeflunomide是抗风湿化合物,是嘧啶合成抑制剂。
MoreTiotropium Bromide hydrate是长效的毒蕈碱受体拮抗剂。
MoreMilrinone是一种有效的,选择性的磷酸二酯酶-3抑制剂,抑制FIII PDE,IC50为0.42 μM。
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