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.
Dovitinib是多靶点RTK抑制剂,对FLT3和c-Kit的IC50分别为1 nM和2 nM,对FGFR1/3和VEGFR1-4的IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2和Dovitinib(CHIR-258; TKI258)是多靶点RTK抑制剂,对FLT3和c-Kit的IC50分别为1 nM和2 nM,对FGFR1/3和VEGFR1-4的IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2和IGFR抑制性较弱。
MoreCHIR-98014是一种有效的GSK-3α/β抑制剂,IC50为0.65 nM/0.58 nM。
MoreVX-765 is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM.
MoreMK-8776 (SCH 900776)是一种选择性Chk1抑制剂,IC50为3 nM,比作用于Chk2选择性高50倍,是高效口服生物相容性的Chk1抑制剂,对Chk2和CDK2的IC50则分别为1500 nM和160 nM。
MoreC646是一种histone acetyltransferase(组蛋白乙酰转移酶)抑制剂,抑制p300,Ki为400 nM,比作用于其他乙酰转移酶选择性高。
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