Synonyms: (S)-pregabalin | CI 1008 | Lyrica® | Nervalin® | PD 144723
pregabalin is an approved drug (FDA and EMA (2004))
Compound class:
Synthetic organic
Comment: Pregabalin is a gabapentinoid class anti-seizure medication. Chemically, it is a 3-isobutyl derivative of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), but it appears to function as a modulator of voltage-gated calcium channels, rather than a GABA receptor agonist.
Ligand Activity Visualisation ChartsThese 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. ✖View more information in the IUPHAR Pharmacology Education Project: pregabalin |
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Bioactivity Comments |
Pregabalin has a reported Kd of 19nM at the pig brain α2δ VGCC [2-3]. We have been unable to find publicly available bioactivity data for this drug at its proposed human molecular target(s) to substantiate its MMOA, and have therefore not tagged a primary drug target. |
Ligand mentioned in the following text fields |
Voltage-gated calcium channels (CaV) overview |