Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 5, 2007, Pages 1200-1205

  Hall, Adrian ^a   Atkinson, Stephen ^a   Brown, Susan H ^a   Chessell, Iain P ^a   Chowdhury, Anita ^a   Giblin, Gerard M P ^a   Goldsmith, Paul ^a   Healy, Mark P ^a   Jandu, Karamjit S ^a   Johnson, Matthew R ^a   Michel, Anton D ^a   Naylor, Alan ^a   Sweeting, Jennifer A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Carboxylic acid replacement; EP1 antagonist; Pyrrole

Indexed keywords

CARBOXYLIC ACID; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; PYRROLE DERIVATIVE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; DRUG BINDING; NONHUMAN;

HUMANS; INHIBITORY CONCENTRATION 50; PROTEIN BINDING; PYRROLES; RECEPTORS, PROSTAGLANDIN E; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33846975119     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.12.021     Document Type: Article

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28. 50 = 5.0 μM at 2C19 isoform.
29. 50 values between 1 and 6 μM; 8f rat CLi 42.0 mL/min/g liver, human CLi >50.0 mL/min/g liver; 8g rat CLi >50.0 mL/min/g liver, human CLi >50.0 mL/min/g liver.
30. 50 values ≥11 μM at 1A2, 2C19, 2C9, 2D6 and 3A4 isoforms; 9f rat CLi 26.0 mL/min/g liver, human CLi 19.0 mL/min/g liver; 9g rat CLi 23.0 mL/min/g liver, human CLi 44.0 mL/min/g liver; 9k rat CLi 32.0 mL/min/g liver, human CLi 26.0 mL/min/g liver.
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