Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit

Journal of Medicinal Chemistry

Volumn 58, Issue 1, 2015, Pages 222-236

  George, Dawn M ^a   Breinlinger, Eric C ^a   Friedman, Michael ^a   Zhang, Yang ^b   Wang, Jianfei ^b   Argiriadi, Maria ^a   Bansal Pakala, Pratima ^a   Barth, Martine ^c   Duignan, David B ^a   Honore, Prisca ^a   Lang, Qingyu ^a   Mittelstadt, Scott ^a   Potin, Dominique ^c   Rundell, Lian ^a   Edmunds, Jeremy J ^a  

^a ABBVIE INC   (United States)

^b WUXI APPTEC   (China)

^c Inventiva   (France)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN KINASE C THETA; PROTEIN KINASE INHIBITOR; ISOENZYME; MOLECULAR LIBRARY; PRKCQ PROTEIN, HUMAN; PROTEIN BINDING; PROTEIN KINASE C;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DISEASE MODEL; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG EFFICACY; DRUG STRUCTURE; DRUG TOLERABILITY; FEMALE; HUMAN; HUMAN CELL; HYPOTHESIS; MALE; MOUSE; NONHUMAN; ANIMAL; ANTAGONISTS AND INHIBITORS; AREA UNDER THE CURVE; ARTHRITIS, EXPERIMENTAL; BAGG ALBINO MOUSE; BIOAVAILABILITY; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; DBA MOUSE; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; METABOLISM; MOLECULAR LIBRARY; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; PHARMACOLOGY; PROTEIN TERTIARY STRUCTURE; RAT; T LYMPHOCYTE; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; ARTHRITIS, EXPERIMENTAL; BIOLOGICAL AVAILABILITY; CELLS, CULTURED; CHROMATOGRAPHY, LIQUID; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG DISCOVERY; FEMALE; HUMANS; ISOENZYMES; MASS SPECTROMETRY; MICE, INBRED BALB C; MICE, INBRED DBA; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN KINASE C; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RATS; SMALL MOLECULE LIBRARIES; T-LYMPHOCYTES;

EID: 84920811206     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500669m     Document Type: Article

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