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.
Adagrasib (MRTX849) 是一种有效的,选择性的和共价的KRAS G12C抑制剂,具有良好的药物样特性,可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导
MoreAtrasentan (ABT-627) 是一种有效的内皮素受体 (endothelin receptor) 拮抗剂,抑制 ETA 的活性,IC50 值为 0.0551 nM.
MoreGepotidacin (GSK2140944) 是一种三氮杂苊烯类化合物,可抑制细菌II型拓扑异构酶。它具有治疗常规病原体和生物威胁病原体的潜力,包括革兰氏阳性菌和耐甲氧西林金黄色葡萄球菌(MRSA)。
MoreTaletrectinib (DS-6051b, AB-106) 是新一代的选择性的ROS1/NTRK 抑制剂,对ROS1,TrkA,TrkB 和TrkC的ic50分别为0.207 nM,0.622 nM,2.28 nM和0.980 nM
MoreVX-548(Suzetrigine)是一种可口服的电压门控钠离子通道 1.8(NaV1.8)高选择性抑制剂,IC50 为 0.7 nM。VX-548可应用于传递痛觉信号、腹壁成形术及拇囊切除术后急性疼痛的研究
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