Chlormezanone exhibits a diverse range of bioactivities and interactions. It shows potency in modulating Lamin A splicing, inhibiting interactions of thyroid hormone receptor and steroid receptor coregulator 2, and inducing erasure of genomic imprints. It is effective in inhibiting the proliferation of Plasmodium falciparum, modulating human peripheral myelin protein 22, and inhibiting several enzymes including human apurinic/apyrimidinic endonuclease 1, MPP8 chromodomain interactions, histone lysine methyltransferase G9a, mammalian selenoprotein thioredoxin reductase 1, and polymerase Iota. Additionally, it inhibits binding or entry into cells for Lassa virus and blocks entry of Ebola virus, while also enhancing Arylsulfatase A activity. The compound shows potential as an inhibitor of sodium fluorescein uptake in OATP1B3-transfected CHO cells and OATP1B1-transfected CHO cells, with high inhibition percentages of 92.0% and 97.47%, respectively.
Chlormezanone demonstrates activity in the FDA HLAED assay related to liver enzyme composite activity and has been assessed for Drug Induced Liver Injury (DILI), being classified as DILI positive. It is associated with various forms of liver toxicity, including acute, cytolytic, and cholestatic liver toxicity, and severe hepatitis, but not with chronic liver diseases or liver tumors.
Despite its broad range of bioactivities, Chlormezanone shows low bioactivity in inhibiting cell viability in Vero E6 cells infected with SARS-CoV-2. It exhibits antiviral activity against SARS-CoV-2 with an IC50 value greater than 20,000 nM. Additionally, it slightly inhibits human HDAC6 enzyme activity and shows binding affinity towards several receptors such as ADRB2, OPRM1, and HRH2, though with no significant inhibitory effects on most targets at concentration levels tested. The compound's wide spectrum of interactions and bioactivities make it a compound of interest for further pharmacological investigation..
Note: Summary generated by AI. Data source: ChEMBL 