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.
PF-543柠檬酸盐是鞘氨醇竞争性的,且可渗透入细胞的SphK1选择性抑制剂,Ki为3.6 nM,对SphK2的抑制性较弱。
MoreAG14361是PARP1抑制剂,Ki<5 nM,比苯甲酰胺的抑制性强1000倍。
More17-AAG (Tanespimycin)是一种有效的HSP90抑制剂,IC50为5 nM,作用于从肿瘤细胞提取的HSP90比作用于从正常细胞提取的HSP90结合亲和力高100倍。
MoreKN-62 is a selective, cell permeable inhibitor of calcium/calmodulin-dependent kinase II (CaMKII; IC50 = 900 nM).
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