MS15 
GtoPdb Ligand ID: 12216
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Synonyms: compound 62 [PMID: 36197750]
Compound class:
Synthetic organic
Comment: MS15 is a PROTAC that targets the AKT serine/threonine kinases for proteasomal degradation [1]. Its AKT binding domain is the allosteric pan-AKT inhibitor miransertib (ARQ-092). This is joined to a von Hippel-Lindau (VHL)-recruiting ligand by a short linker. MS15 selectively and significantly degrades AKT1 and AKT2 and suppresses proliferation in cancer cells with KRAS/BRAF mutations. AKT3 is expressed at very low levels in the SW620 cells used in the assay, so the degrading effect of MS15 on AKT3 is unclear. An earlier AKT-directed PROTAC (MS21) with an ATP-competitive AKT inhibitor (capivasertib/AZD5363) as warhead was not anti-proliferative against KRAS/BRAF mutation-carrying cells.
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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