Triamino pyrimidines and pyridines as histamine H4 receptor modulators

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 10, 2011, Pages 3113-3116

  Meduna, Steven P ^a   Savall, Brad M ^a   Cai, Hui ^a   Edwards, James P ^a   Thurmond, Robin L ^a   McGovern, Patricia M ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Antagonist; Histamine; Histamine H4; Pyridine; Pyrimidine

Indexed keywords

HISTAMINE H4 RECEPTOR; PYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; PYRIMIDINETRIAMINE; TRIAMINOPYRIDINE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION;

AMINES; BINDING, COMPETITIVE; BIOLOGICAL ASSAY; HUMANS; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PROTEIN BINDING; PYRIDINES; PYRIMIDINES; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79955566558     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.017     Document Type: Article

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10. 2) and incubated at room temperature for 10 min. Cells are then incubated with 100 μL of 1× assay buffer including 0.5% Triton X-100 and 40 mM B mercaptoethanol for 10 min. 25 μL of substrate solution (1 mg/mL chlorophenolred B-D galactopyranoside) was added and the color was quantitated at an absorbance of 570 nm. α values are calculated using the full agonist (positive control) as the standard of 1.