Discovery of 9-Cyclopropylethynyl-2-((<i>S</i>)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-<i>a</i>]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
第一作者:
Frédéric,Labéguère
第一单位:
Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France.
作者:
医学主题词
乙酸盐类(Acetates);别构调节(Allosteric Regulation);动物(Animals);Caco-2细胞(Caco-2 Cells);细胞, 培养的(Cells, Cultured);狗(Dogs);药物发现(Drug Discovery);药物评价, 临床前(Drug Evaluation, Preclinical);女(雌)性(Female);HEK293细胞(HEK293 Cells);人类(Humans);男(雄)性(Male);小鼠(Mice);小鼠, 近交BALB C(Mice, Inbred BALB C);微粒体, 肝(Microsomes, Liver);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);受体, G-蛋白偶联(Receptors, G-Protein-Coupled)
DOI
10.1021/acs.jmedchem.0c00272
PMID
32902984
发布时间
2020-12-31
- 浏览3
Journal of medicinal chemistry
13526-13545页
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