Synonyms: 10-DEBC | NCGC00167772-01
Compound class:
Synthetic organic
Comment: This is compound 10B in [4] which describes its actions as an Akt (aka protein kinase B) inhibitor.
This compound is a thioridazine derivative. Thioridazine is a well known antipsychotic that acts as an antagonist of dopamine receptor activity. The compound also inhibits the kinase activity of Pim-1 [3] and X-ray crystallography shows the compound binding to the Pim-1 pharmacophore. ![]() 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. ✖ |
|
Bioactivity Comments |
Using recombinant human Akt1 (PKBα) and phosphorylation of downstream GSK-3β as a readout of Akt1 activity, Thimmaiah et al (2005) show that this compound almost completely blocks Akt activity at 5μM (see Figure 6 in the article) [4]. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||
|