A947 
GtoPdb Ligand ID: 12308
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Compound class:
Synthetic organic
Comment: A947 is a selective degrader of SMARCA2 [1]. It is a PROTAC class molecule that targets SMARCA2 protein for degradation via ligation with the VHL E3 ubiquitin ligase. Its target protein binding component interacts with the bromodomains of SMARCA2 and -4 and the 5th bromodomain of polybromo 1 (PBRM1). A947 was developed by Arvinas/Genentech to assess the utility of targeting SMARCA2 in SMARCA4-mutated cancers that become dependent on the SMARCA2 paralog for survival.
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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