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Volumn 16, Issue 16, 2006, Pages 4339-4344

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: Identification of candidates for clinical development

Author keywords

Anti inflammatory; Arthritis; Clinical candidate; CP 808844; Cytokine; Inflammation; Inhibitor; MAP; mitogen activated protein; Oxazole; p38 kinase; SAR; structure activity relationship; TNF ; Triazole; Triazolopyridine; tumor necrosis factor

Indexed keywords

CP 808844; OXAZOLE DERIVATIVE; PROTEIN INHIBITOR; PROTEIN P38 INHIBITOR; UNCLASSIFIED DRUG;

EID: 33745699202     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.05.056     Document Type: Article
Times cited : (30)

References (25)
  • 6
    • 33745718489 scopus 로고    scopus 로고
    • note
    • 2 for 4 h. Plasma was assessed for TNF-α by ELISA (R&D Systems).
  • 14
    • 33745704453 scopus 로고    scopus 로고
    • note
    • 50s > 10 μM against the following kinases: p38γ, p38δ, MKK1, MAPK2/ERK2, JNK, MAPKAP-K1a, MAPKAP-K2, MSK1, PRAK, PKA, PKCα, PDK1, PKBα, SGK, P70S6K, GSK3β, ROCK-II, AMPK, CHK1, CK2, Lck, CSK, CDK2, PI3-K, DYRK1a, PHOS. Kinase.
  • 15
    • 33745718487 scopus 로고    scopus 로고
    • note
    • All procedures were reviewed and approved by the Institutional Animal Care & Use Committee.
  • 16
    • 33745732470 scopus 로고    scopus 로고
    • note
    • 2 and bled by cardiac puncture. Blood was collected in Vaccutainer tubes and spun for 20 min at 3000 rpm. Serum was assayed for TNF-α levels using an ELISA (R& D Systems).
  • 17
    • 33745690241 scopus 로고    scopus 로고
    • Kalgutkar, A. S.; Hatch, H. L.; Kosea, F.; McClure, K. F.; Dombroski, M. A.; Choo, E. F.; Henne, K. R.; Taylor, T. J.; Kuperman, A. V. Boopharm. Drug Dispos. Manusscript in press.
  • 18
    • 33745718486 scopus 로고    scopus 로고
    • note
    • PDB accession code 1ZZL.
  • 19
    • 33745718483 scopus 로고    scopus 로고
    • note
    • 2. After 4 h, cell supernatants were harvested by centrifugation and TNF-α concentration determined by ELISA (R&D).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.