Route to Prolonged Residence Time at the Histamine H(1) Receptor: Growing from Desloratadine to Rupatadine

[Image: see text] Drug–target binding kinetics are an important predictor of in vivo drug efficacy, yet the relationship between ligand structures and their binding kinetics is often poorly understood. We show that both rupatadine (1) and desloratadine (2) have a long residence time at the histamine...

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Bibliografiska uppgifter
I publikationen:J Med Chem
Huvudupphovsmän: Bosma, Reggie, Wang, Zhiyong, Kooistra, Albert J., Bushby, Nick, Kuhne, Sebastiaan, van den Bor, Jelle, Waring, Michael J., de Graaf, Chris, de Esch, Iwan J., Vischer, Henry F., Sheppard, Robert J., Wijtmans, Maikel, Leurs, Rob
Materialtyp: Artigo
Språk:Inglês
Publicerad: American Chemical Society 2019
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC6750840/
https://ncbi.nlm.nih.gov/pubmed/31274307
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00447
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