4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.

Liddle, John; Bamborough, Paul; Barker, Michael D; Campos, Sebastien; Chung, Chun-Wa; Cousins, Rick P C; Faulder, Paul; Heathcote, Michelle L; Hobbs, Heather; Holmes, Duncan S; Ioannou, Chris; Ramirez-Molina, Cesar; Morse, Mary A; Osborn, Ruth; Payne, Jeremy J; Pritchard, John M; Rumsey, William L; Tape, Daniel T; Vicentini, Giorgia; Whitworth, Caroline; Williamson, Rick A

Liddle, John; Bamborough, Paul; Barker, Michael D; Campos, Sebastien; Chung, Chun-Wa; Cousins, Rick P C; Faulder, Paul; Heathcote, Michelle L; Hobbs, Heather; Holmes, Duncan S; Ioannou, Chris; Ramirez-Molina, Cesar; Morse, Mary A; Osborn, Ruth; Payne, Jeremy J; Pritchard, John M; Rumsey, William L; Tape, Daniel T; Vicentini, Giorgia; Whitworth, Caroline; Williamson, Rick A.

Affiliation

Liddle J; GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. john.2.liddle@gsk.com

Bioorg Med Chem Lett ; 22(16): 5222-6, 2012 Aug 15.

Article in En | MEDLINE | ID: mdl-22801646

Subject(s)

I-kappa B Kinase/antagonists & inhibitors; Indoles/chemistry; Protein Kinase Inhibitors/chemistry; Animals; Biological Availability; Disease Models, Animal; Half-Life; Humans; I-kappa B Kinase/metabolism; Indoles/chemical synthesis; Indoles/pharmacokinetics; Lung/metabolism; Neutrophils/immunology; Neutrophils/metabolism; Protein Kinase Inhibitors/chemical synthesis; Protein Kinase Inhibitors/pharmacokinetics; Rats; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase Inhibitors / I-kappa B Kinase / Indoles Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Type: Article Affiliation country: United kingdom

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