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Volumn 19, Issue 9, 2009, Pages 2524-2529

3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization

Author keywords

Carbamate; mGluR2; Positive allosteric modulator; Schizophrenia

Indexed keywords

EGLUMETAD; METABOTROPIC RECEPTOR 2; OXAZOLIDINE DERIVATIVE;

EID: 64249109525     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.032     Document Type: Article
Times cited : (29)

References (30)
  • 17
    • 64249136761 scopus 로고    scopus 로고
    • note
    • MS-based quantification of the basal/apical transfer rate of a test compound at 2 μM across contiguous monolayers from MDCK (Madin Darby Canine Kidney) cells.
  • 18
    • 64249088874 scopus 로고    scopus 로고
    • note
    • Ratio from the MS-based quantification of apical/basal and basal/apical transfer rates of a test compound at 2 μM across contiguous monolayers from MDR1-transfected MDCK cells.
  • 20
    • 64249120864 scopus 로고    scopus 로고
    • note
    • 50 value depends on the concentration of glutamate present in the assay, the precise assessment of the ligand efficiency based on this assay was not possible. At the same time, comparison of LE profiles of multiple chemotypes using the same mGluR2 assay provided a valuable perspective when assessing lead generation potential of different chemical series.
  • 25
    • 64249135404 scopus 로고    scopus 로고
    • note
    • Fluorescence-based measurement of CYP inhibition by incubating the recombinant CYP (Cytochrome P450) with a test compound and the corresponding fluorescent probe at 3 μM.
  • 26
    • 64249084672 scopus 로고    scopus 로고
    • note
    • 3H-dofetilide binding to membranes from hERG-expressing HEK cells at 10 μM.
  • 27
    • 64249141114 scopus 로고    scopus 로고
    • note
    • In efforts to obtain analogs in solid form, we compared the MPs of small alkoxyphenyl ethers (oils) to benzylphenyl ether (∼40 °C), phenyl ether (∼28 °C) and biphenyl (∼70 °C).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.