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.
D 4476 是一种有效的,选择性的,细胞渗透性 CK1 (casein kinase 1) 抑制剂,无细胞测定中对来自粟酒裂殖酵母的 CK1 和 CK1δ,IC50 分别为 200 nM 和 300 nM 。也是一种 ALK5 抑制剂,IC50 为 500 nM。
MoreNSC-405020是MT1-MMP抑制剂,能特异地靶向MT1-MMP的PEX结构域,不会抑制MT1-MMP和MMP-2的催化活性。
MoreA-966492是一种新型有效的PARP1和PARP2抑制剂,Ki分别为1 nM和1.5 nM。
MoreAZD8330是一种新型,选择性的,非ATP竞争性MEK 1/2抑制剂,IC50为7 nM。
MoreNVP-HSP990是Hsp90抑制剂,对Hsp90α的IC50值为13nM,抗癌增殖活性。
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