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.
Afatinib (BIBW2992)是一种不可逆EGFR/HER2抑制剂,对EGFR(wt), EGFR(L858R), EGFR(L858R/T790M)和HER2均有抑制作用,IC50分别为0.5 nM,0.4 nM,10 nM和14 nM;用于Gefitinib抗性的突变型EGFR (L858R-T790M )时,活性增强100倍。
MoreMaraviroc是一种趋化因子受体CCR5抑制剂,作用于MIP-1α, MIP-1β和RANTES 时,IC50分别为3.3 nM, 7.2 nM和5.2 nM。
MoreCYT387是一种ATP竞争性JAK1/JAK2抑制剂,IC50为11 nM/18 nM,比作用于JAK3选择性约高10倍左右。
MoreLY364947(HTS466284)是TGF(beta)R-I高效ATP竞争性抑制剂,IC50值为59nM,对TGF(beta)R-II的抑制活性弱7倍。
MoreBIX 02189是一种选择性的MEK5抑制剂,IC50为1.5 nM,也抑制ERK5催化活性,IC50为810 nM,且不抑制与其密切相关的激酶MEK1, MEK2, ERK2,和JNK2。
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