Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
第一作者:
Timothy D,Cushing
第一单位:
Department of Therapeutic Discovery, ‡Department of Pharmacokinetics and Drug Metabolism, and §Department of Pharmaceutics Research and Development, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
作者:
医学主题词
腺苷(Adenosine);动物(Animals);自身免疫疾病(Autoimmune Diseases);细胞, 培养的(Cells, Cultured);I类磷脂酰肌醇3-激酶类(Class I Phosphatidylinositol 3-Kinases);结晶学, X线(Crystallography, X-Ray);疾病模型, 动物(Disease Models, Animal);药物发现(Drug Discovery);女(雌)性(Female);人类(Humans);炎症(Inflammation);小鼠, 近交BALB C(Mice, Inbred BALB C);小鼠, 转基因(Mice, Transgenic);模型, 化学(Models, Chemical);模型, 分子(Models, Molecular);分子结构(Molecular Structure);蛋白质结合(Protein Binding);蛋白激酶抑制剂(Protein Kinase Inhibitors);蛋白质结构, 三级(Protein Structure, Tertiary);喹啉类(Quinolines);大鼠, 近交Lew(Rats, Inbred Lew);构效关系(Structure-Activity Relationship)
DOI
10.1021/jm501624r
PMID
25469863
发布时间
2018-07-26
- 浏览55
Journal of medicinal chemistry
480-511页
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