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.
Rucaparib phosphate是PARP抑制剂,对PARP1的Ki为1.4 nM,对PARP其余亚型也有亲和性。
MoreGSK J4 hydrochloride is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.
MoreLY2228820是p38MAPK抑制剂,对p38αMAPK和p38βMAPK的IC50分别为7 nM和3 nM。
MoreSitagliptin(MK 0431)是DPP4高效抑制剂,在Caco-2细胞中IC50值为19nM。
MoreTofacitinib (CP-690550) Citrate是一种新型JAK3抑制剂,IC50为1 nM,作用于JAK2和JAK1选择性比其低20到100倍。
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