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.
TG-101348 (SAR302503)是JAK2选择性抑制剂,IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,同时还能抑制BRD4,IC50为340 nM。
MoreNLG919是一种新型有效的indoleamine-2,3-dioxygenase (IDO)(吲哚胺-2,3-双加氧酶)抑制剂,EC50为75 nM。
MoreBGJ398 (NVP-BGJ398)是一种选择性的FGFR抑制剂,作用于FGFR1/2/3,IC50为0.9 nM/1.4 nM/1 nM,作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上,对Abl, Fyn, Kit, Lck, Lyn和Yes几乎没有抑制活性。
MoreValproic acid sodium salt (Sodium valproate)是一种HDAC抑制剂,IC50为0.4 mM,也抑制GABA-转氨酶或琥珀酸半醛脱氢酶。
MoreLosmapimod一种是口服活性的p38 MAPK抑制剂,对p38α和p38β的pKi为8.1和7.6。
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