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.
AZD1480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。
MoreVX-702是一种高选择性p38α MAPK抑制剂,作用于p38α比作用于p38β效果高14倍。
MoreNPS-2143是一种新型有效的,选择性的Ca(2+)受体拮抗剂,IC50为43 nM。
MoreRuxolitinib (INCB018424)是选择性的JAK1/2抑制剂,IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与 作用于JAK3相比,选择性强130倍多。
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