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.
GSK343是一种选择性EZH2抑制剂,IC50为4 nM,比作用于EZH1选择性高60倍,比作用于其他组蛋白甲基转移酶选择性高1000倍以上。
MoreEX 527 (Selisistat)是一种有效的,选择性的SIRT1抑制剂,IC50为38 nM,比作用于SIRT2和SIRT3选择性高200倍以上。
MoreNiclosamide, an FDA approved anthelmintic drug, is an inhibitor of Wnt co-receptor LRP6 and suppresses both the Wnt/β-catenin pathways and the mTOR/STAT3 pathway. Niclosamide抑制DNA复制,抑制STAT,IC50为0.7 μM。
MoreGDC-0994 is a potent, orally available ERK inhibitor with IC50 1.1 nM and 0.3 nM, respectively.
MoreGSK3787 is a selective and irreversible PPARβ/δ antagonist with good pharmacokinetic properties. GSK3787是不可逆的PPARδ选择性拮抗剂,pIC50为6.6,对hPPARα和hPPARγ无亲和力。
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