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.
Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂,IC50为1 nM,作用于JAK2和JAK1选择性低20到100倍。
MoreCanertinib (CI-1033)是一种pan-ErbB抑制剂,同时抑制EGFR和ErbB2,IC50分别为1.5 nM和9.0 nM,但对PDGFR, FGFR, InsR, PKC,和CDK1/2/4等均无抑制活性。
MoreFinasteride是口服活性的睾酮5α-还原酶抑制剂,Ki为10 nM。
MoreBIX 01294是一种G9ahistone methyltransferase(组蛋白甲基转移酶)抑制剂,IC50为2.7 μM,降低组蛋白H3K9me2,也能微弱抑制GLP(主要是H3K9me3),对其他组蛋白甲基转移酶没有显著的抑制活性。
MoreGenistein是一种来源于大豆的植物雌激素,是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂,在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂,IC50分别为12μM和19 μM。
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