Synonyms: CTX-3648 | CTx-648 | PF9363
Compound class:
Synthetic organic
Comment: PF-9363 (CTx-648) is an oral and selective KAT6A/B inhibitor that blocks histone H3K23 acetylation (H3K23Ac; IC50 <1 nM) [2]. Inhibition of histone acetyltransferases KAT6A/B induces senescence and arrests tumour growth [1].
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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References |
1. Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y et al.. (2018)
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature, 560 (7717): 253-257. [PMID:30069049] |
2. Sharma S, Chung CY, Uryu S, Petrovic J, Cao J, Rickard A, Nady N, Greasley S, Johnson E, Brodsky O et al.. (2023)
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer. Cell Chem Biol, 30 (10): 1191-1210.e20. [PMID:37557181] |