Synonyms: FX-1006 | Vyndamax® | Vyndaqel®
tafamidis is an approved drug (EMA and UK (2011), FDA (2019))
Compound class:
Synthetic organic
Comment: Tafamidis binds potently and selectively to transthyretin (TTR), stabilising protein tetramers, thereby inhibiting the formation of amyloid fibrils [2]. The trade name for this drug is Vyndaqel which contains tafamidis meglumine (PubChem CID 24970412). The Vyndamax brand contains tafamidis parent molecule.
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. ✖ |
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Bioactivity Comments |
Tafamidis binds within the thyroxine-binding sites of the TTR complex to stabilise the tetrameric structure [2]. It is able to stabilise wild-type and mutated TTR structures [5]. Information from X-ray crystal structures indicates that tafamidis stabilises the interaction between the two identical homodimers which form the tetrameric TTR complex. The dimer-dimer interaction is a relatively weak association and is the first to fail in tetramer dissociation [3]. |
Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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Ligand mentioned in the following text fields |
Transthyretin overview |