- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: XAP044 exerts antagonist-like activity at the mGlu5 receptor, binding to a novel site within the extracellular Venus flytrap domain compared with known selective ligands , making this compound a negative allosteric modulator (NAM).
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. Gee CE, Peterlik D, Neuhäuser C, Bouhelal R, Kaupmann K, Laue G, Uschold-Schmidt N, Feuerbach D, Zimmermann K, Ofner S et al.. (2014)
Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior.
J Biol Chem, 289 (16): 10975-87. [PMID:24596089]