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.
Lovastatin (洛伐他汀) 是高效HMG-CoA还原酶抑制剂,IC50为3.4 nM,有降血脂作用。
MoreDAPT (GSI-IX)是新型γ-分泌酶抑制剂,抑制HEK 293细胞中全部Aβ, IC50为20 nM。
MoreSB525334是一种有效的,选择性的TGFβ receptor I (ALK5)抑制剂,IC50为14.3 nM,作用于ALK4比作用于ALK5效果低4倍,可抑制ALK2, 3,和6活性。
MoreBaricitinib是JAK1和JAK2抑制剂,IC50分别为5.9 nM和5.7 nM,比对JAK3和Tyk2的抑制性高70倍和10倍,对c-Met和Chk2无活性。
MoreEPZ5676是蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂,Ki为80 pM,比作用于所有其他PMTs选择性高37,000以上,抑制肿瘤H3K79甲基化。
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