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Synonyms: compound 28 [PMID: 29470065] | VUF 14738 | VUF-14738
Compound class: Synthetic organic
Comment: VUF14738 is a bidirectional photo-switchable histamine H3 receptor antagonist based on the structure of compound 3a [PMID: 18606542] . The chemical structure shown here is the photo-activated isomer that binds the H3 receptor under UV illumination. VUF14738 binding is 'switched-on' by UV light. VUF14738 swiftly and reversibly photoisomerizes (via trans/cis conversion) and is suitable for spatiotemporal studies of H3 receptor signaling. See also VUF14862, which operates in the opposite direction.
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. Hauwert NJ, Mocking TAM, Da Costa Pereira D, Kooistra AJ, Wijnen LM, Vreeker GCM, Verweij EWE, De Boer AH, Smit MJ, De Graaf C et al.. (2018)
Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology.
J Am Chem Soc, 140 (12): 4232-4243. [PMID:29470065]