Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.
第一作者:
Sharan K,Bagal
第一单位:
Worldwide Medicinal Chemistry , Pfizer Global R&D U.K. , The Portway Building, Granta Park , Cambridge CB21 6GS , U.K.
作者:
主题词
别构调节(Allosteric Regulation);氨基酸序列(Amino Acid Sequence);动物(Animals);结合部位(Binding Sites);结晶学, X线(Crystallography, X-Ray);药物评价, 临床前(Drug Evaluation, Preclinical);半衰期(Half-Life);高通量筛选分析(High-Throughput Screening Assays);人类(Humans);配体(Ligands);微粒体, 肝(Microsomes, Liver);分子动力学模拟(Molecular Dynamics Simulation);蛋白质结合(Protein Binding);蛋白质亚型(Protein Isoforms);蛋白激酶抑制剂(Protein Kinase Inhibitors);蛋白质结构, 三级(Protein Structure, Tertiary);吡唑类(Pyrazoles);大鼠(Rats);受体, trkA(Receptor, trkA);序列比对(Sequence Alignment);构效关系(Structure-Activity Relationship)
DOI
10.1021/acs.jmedchem.8b00280
PMID
29672039
发布时间
2019-10-14
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Journal of medicinal chemistry
247-265页
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