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Volumn 20, Issue 20, 2010, Pages 6108-6115

Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization

Author keywords

3 Adrenergic receptor; Adrenoceptor; GPCR; Molecular modeling; vHTS

Indexed keywords

ARYLOXYPROPANOLAMINE; BETA 3 ADRENERGIC RECEPTOR STIMULATING AGENT; LEAD; PROPANOLAMINE DERIVATIVE; PYRIMIDINE; THIENOPYRIMIDINE; UNCLASSIFIED DRUG;

EID: 77956896566     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.039     Document Type: Article
Times cited : (8)

References (29)
  • 10
    • 77956920531 scopus 로고    scopus 로고
    • note
    • All aryloxypropanolamine derivatives were tested as racemates. For a further lead optimization process, the (S)-enantiomers proved to be more active than the respective (R)-enantiomers.
  • 11
    • 77956936783 scopus 로고    scopus 로고
    • note
    • 50 determinations, which were based on concentration curves using eight concentrations (half-logarithmic) in duplicate.
  • 12
    • 77956906085 scopus 로고    scopus 로고
    • note
    • 50 values, respectively, were determined by dose-response curves based on seven concentrations (logarithmic) determined in duplicate.
  • 13
    • 77956924713 scopus 로고    scopus 로고
    • note
    • The term 'affinity' is strictly used for the description of binding data, whereas 'activity' refers to functional data from cellular assays throughout this Letter.
  • 19
    • 77956902705 scopus 로고    scopus 로고
    • note
    • Chlorothienopyrimidines 6 are commercially available, except for 4-chloro-5-phenylthieno[2,3-d]pyrimidine, cf. Supplementary data.
  • 23
    • 77956912271 scopus 로고    scopus 로고
    • https://pharmacology.ricerca.com/Catalog/AssayCatalog/AssayCatalog.aspx, than 'Molecular Packages'.
  • 24
    • 77956944393 scopus 로고    scopus 로고
    • Program packages MOE and Maestro/QikProp
    • Program packages MOE and Maestro/QikProp.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.