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.
Limonin为柑橘类水果中富含的三萜类化合物,具有抗病毒和抗肿瘤活性。
MorePFI-2是甲基转移酶SETD7高效选择性抑制剂,IC50值为2nM。
MoreSB-743921是第二代高活性KSP抑制剂,Ki为0.1 nM,对MKLP1,Kin2,Kif1A,Kif15,KHC,Kif4和CENP-E无亲和力。
MoreTDZD-8是一种非ATP竞争性GSK-3β抑制剂,IC50为2 μM;对CDK1, casein kinase II, PKA和PKC具有最低限度的抑制效果。
MoreResminostat是HDAC1/3/6抑制剂,IC50为43到72 nM,而对HDAC8的IC50为877 nM。
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