Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 19, 2015, Pages 4109-4113

  Fauber, Benjamin P ^a   Gobbi, Alberto ^a   Savy, Pascal ^b   Burton, Brenda ^b   Deng, Yuzhong ^a   Everett, Christine ^a   La, Hank ^a   Johnson, Adam R ^a   Lockey, Peter ^b   Norman, Maxine ^b   Wong, Harvey ^a  

^a GENENTECH INC   (United States)

^b Argenta Discovery Ltd   (United Kingdom)

Author keywords

Autoimmune; IL 17; Inflammation; RORc; ROR

Indexed keywords

AGENTS AFFECTING METABOLISM; INTERLEUKIN 17; QUINOLINE DERIVATIVE; RETINOIC ACID RECEPTOR RELATED ORPHAN RECEPTOR C ANTAGONIST; SULFONE DERIVATIVE; UNCLASSIFIED DRUG; N-SULFONYL-TETRAHYDROQUINOLINE; RETINOID RELATED ORPHAN RECEPTOR GAMMA; RORC PROTEIN, HUMAN;

ANIMAL CELL; ANTAGONIST POTENCY; APPARENT PERMEABILITY; ARTICLE; BIOCHEMICAL ANALYSIS; CELL ASSAY; CRYSTAL STRUCTURE; CYTOKINE PRODUCTION; DRUG ACTIVITY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SYNTHESIS; EC50; HEPATIC CLEARANCE; HUMAN; HUMAN CELL; HYDROGEN BOND; IN VITRO STUDY; LIGAND BINDING; LIVER MICROSOME; METABOLIC STABILITY; MOLECULAR MODEL; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PLASMA PROTEIN BINDING; STRUCTURE ACTIVITY RELATION; AGONISTS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; INVERSE AGONISM; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INVERSE AGONISM; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84945493631     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.08.028     Document Type: Article

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