Ligand based design of novel histamine H 4 receptor antagonists; Fragment optimization and analysis of binding kinetics

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 461-467

  Smits, Rogier A ^a   Lim, Herman D ^a   Van Der Meer, Tiffany ^a   Kuhne, Sebastiaan ^a   Bessembinder, Karin ^a   Zuiderveld, Obbe P ^a   Wijtmans, Maikel ^a   De Esch, Iwan J P ^a   Leurs, Rob ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

Author keywords

Binding kinetics; Fragment optimization; GPCR; H 4R antagonist; Histamine

Indexed keywords

1 (5 CHLORO 2 BENZIMIDAZOLYLCARBONYL) 4 METHYLPIPERAZINE; 1 (5 CHLORO 2 INDOLYLCARBONYL) 4 METHYLPIPERAZINE; 7 (FURAN 2 YL) 4 (PIPERAZIN 1 YL)QUINAZOLIN 2 AMINE; HISTAMINE H4 RECEPTOR ANTAGONIST; ISOQUINOLINE; QUINAZOLINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BINDING KINETICS; DRUG BIOAVAILABILITY; DRUG HALF LIFE; HUMAN; HUMAN CELL; LIGAND BINDING; MOUSE; NONHUMAN;

ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HISTAMINE ANTAGONISTS; HUMANS; HYPERSENSITIVITY; INHIBITORY CONCENTRATION 50; KINETICS; LIGANDS; MICE; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR CONFORMATION; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS;

EID: 84655162331     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.104     Document Type: Article

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