Synonyms: CBPD268 | compound 33 [PMID: 38477974]
Compound class:
Synthetic organic
Comment: CBPD-268 is an orally bioactive CBP/p300 PROTAC degrader [1]. The target protein binding component is based on the chemical structure of the CBP/p300 bromodomain inhibitor GNE-049. A new cereblon-binding ligand (TX-16; compound 27 in [2]) is incorporated to engage the E3 ubiquitin ligase.
CBP and p300 are transcriptional coactivators of the androgen receptor (AR) that are found to be abberantly expressed in prostate cancer, and to confer resistance to AR-targeted prostate cancer therapies. CBPD-268 is therefore proposed as an anti-prostate cancer strategy. 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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