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

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 16, 2012, Pages 5222-5226

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

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Azaindole; IKK2; Kinase

Indexed keywords

4 PHENYL 7 AZAINDOLE DERIVATIVE; ADENOSINE TRIPHOSPHATE; I KAPPA B KINASE; I KAPPA B KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; IN VIVO STUDY; LIPOPHILICITY; NEUTROPHIL; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BIOLOGICAL AVAILABILITY; DISEASE MODELS, ANIMAL; HALF-LIFE; HUMANS; I-KAPPA B KINASE; INDOLES; LUNG; NEUTROPHILS; PROTEIN KINASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84864412625     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.06.065     Document Type: Article

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