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.
Apremilast是一种口服生物有效的PDE4和TNF-α抑制剂,IC50分别为74 nM和77 nM。
MorePP-121是多靶点抑制剂,对于PDGFR,Hck,mTOR,VEGFR2,Src和Abl的IC50分别为2 nM,8 nM,10 nM,12 nM,14 nM和18 nM,同时还可抑制DNA-PK(IC50为60 nM)。
MoreCiproxifan是高活性的H3受体拮抗剂,IC50为9.2 nM,对其它亚型受体的亲和力较低。
MoreRefametinib是口服生物相容性的MEK抑制剂,对MEK1和MEK2的IC50分别为19 nM和47 nM,有抗肿瘤活性。
MoreGossypol具有抗癌,抗炎活性,能结合Bcl-2。
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