ICI 204,448 exhibits a diverse range of bioactivities, indicating its potential in various biological contexts. Specifically, it acts as a general anesthetic with a potency of 50118.7 nM and demonstrates differential inhibition of Plasmodium falciparum proliferation with potencies ranging from 12589.3 nM to 15848.9 nM. It is a potent inhibitor of Tau fibril formation at 177.8 nM and Human Peripheral Myelin Protein 22 expression/activity at 95283.4 nM. It inhibits histone lysine methyltransferase G9a at 10000.0 nM and 17782.8 nM, functions as an antagonist of the Neuropeptide S Receptor with a potency of 31622.8 nM, and inhibits AmpC Beta-Lactamase at 5011.9 nM. Additionally, it interacts with MPP8 Chromodomain (177.8 nM), inhibits HP1-beta Chromodomain (89125.1 nM), mammalian selenoprotein Thioredoxin Reductase 1 (946.6 nM), ERG Ets/DNA interaction (11220.2 nM), and PLK1-PDB (67015.8 nM).
In cell viability assays, compound 705742 shows mixed effects on HEK293T and U2OS cells, with growth rates of 0.0 and 1.0, while consistently inhibiting human fibroblast cells (growth rate of 0.0). Thermal Shift Assays reveal that the compound can both stabilize and destabilize protein structures, indicated by varied Delta TM values.
In GPCR beta-arrestin recruitment assays, ICI 204,448 displays both agonistic and inhibitory effects across multiple receptors, including APLNR, C5AR1, FPR2, S1PR1, ADRB2, GPR119, ADGRF1, CX3CR1, FFAR4, ADRA2A, GLP1R, GPR35, and AGTR1, at a concentration of 0.00001. These complex interactions underline the compound’s multifaceted bioactivity and warrant further investigation for its potential therapeutic applications..
Note: Summary generated by AI. Data source: ChEMBL 