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Synonyms: Bilaxten® | Ilaxten®
bilastine is an approved drug (UK (2010))
Compound class: Synthetic organic
Comment: Bilastine is a non-sedating histamine H1 receptor antagonist/inverse agonist [2-3]. A repurposing screen of small molecule drugs discovered that bilastine inhibits SARS-CoV-2 Mpro activity by around 20% (see CHEMBL4495564).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A. (2005)
Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity.
Drugs R D, 6 (6): 371-84. [PMID:16274260]
2. Sharma S, Hatware K, Bhadane P, Patil K. (2021)
Chemistry, Pharmacokinetics, Pharmacodynamics and Analytical Methods of Bilastine, a Histamine H1 Receptor Antagonist: An Update.
Mini Rev Med Chem, 21 (20): 3183-3190. [PMID:33992058]
3. Wolthers OD. (2013)
Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.
Biomed Res Int, 2013: 626837. [PMID:23956994]