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.
Sotrastaurin(AEB-071)是PKCθ选择性抑制剂,Ki为0.22 nM。
MoreFilgotinib (GLPG0634) is the first selective inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
MoreLDN193189 HCl是LDN193189的盐酸盐,这是一种选择性BMP信号抑制剂,它能抑制BMP type I receptors ALK2和ALK3的转录活性,其 IC50 为 5 nM 和 30 nM, 并且对于BMP的选择性是对TGF-β选择性的200倍。
MoreAZD1480是一种新型,ATP竞争性的JAK2抑制剂,IC50为0.26 nM,选择性作用于JAK3和Tyk2,对JAK1的作用较弱。
MoreHydrocortisone (氢化可的松) 为主要的糖皮质素,由肾上腺皮质分泌。
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