Synonyms: BMN-673 | BMN673 | Talzenna®
talazoparib is an approved drug (FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Talazoparib is a PARP inhibitor [8], inhibiting both PARP1 and PARP2 [1,8]. The compound is bioavailable as the tosylate salt (PubChem CID 56966514).
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 |
Talazoparib is claimed in patent US8012976, and whilst the patent provides generalised comment on the IC50s of example compounds, specific values are not provided. IC50 values ranged from <5nM to 50nM in chemiluminescent enzyme assays. We have tagged PARP1 and PARP2 as the primary targets of this compound based on the crystallisation report of the compound bound to the catalytic domain of each enzyme [1]. |
Selectivity at enzymes | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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