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Volumn 21, Issue 1, 2011, Pages 417-422

A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit

(34)  Cushing, Timothy D a   Baichwal, Vijay a   Berry, Karen a   Billedeau, Roland b   Bordunov, Viola b   Broka, Chris b   Cardozo, Mario a   Cheng, Peng a   Clark, David a   Dalrymple, Stacie c   Degraffenreid, Michael a   Gill, Adrian b   Hao, Xiaolin a   Hawley, Ronald C b   He, Xiao a   Jaen, Juan C a   Labadie, Sharada S b   Labelle, Marc a   Lehel, Csaba a   Lu, Pu Ping a   more..


Author keywords

IKK ; IKK ; Semicarbazones; Semithiocarbazones

Indexed keywords

IMIDAZOLE; PROTEIN SERINE THREONINE KINASE INHIBITOR; QUINOLINE; THIOSEMICARBAZONE DERIVATIVE;

EID: 78650514545     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.126     Document Type: Article
Times cited : (13)

References (37)
  • 12
    • 78650517003 scopus 로고    scopus 로고
    • Note
    • Millennium (Takeda) had entered MLN-0415 a small molecule inhibitor of IKKβ in a phase I study in 2006. The structure has not yet been disclosed.
  • 23
    • 78650511808 scopus 로고    scopus 로고
    • Callahan, J. F; Kerns, J. K.; Lin, X. PCT Int. Appl. WO 2007102883.
    • Callahan, J. F; Kerns, J. K.; Lin, X. PCT Int. Appl. WO 2007102883.
  • 34
    • 78650514146 scopus 로고    scopus 로고
    • note
    • 50s were determined by curve fitting with LSW data analysis software (MDL).
  • 35
    • 0028168798 scopus 로고    scopus 로고
    • note
    • NF-kB gel shift assays were carried out as described (Schindler, U.; Baichwal, V. R. Mol. Cell Biol. 1994, 14, 5820). In summary, IL8/ECV304 cells were stimulated with TNF for 1 h in the absence or presence of compounds and NF-kB. DNA binding activity was determined by gel shift experiments from crude nuclear extracts.
  • 36
    • 78650512290 scopus 로고    scopus 로고
    • note
    • Human whole blood assay: blood samples in a 96-well microtiter plate were stimulated for 5 h with LPS in the presence or absence of test compounds. Following the incubation period, levels of TNF in the culture supernatants were determined with an ELISA kit (R&D systems).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.