Alternative Targets and Therapeutics

Application Note

Identifying a Polypharmacological Profile for Phenothiazines

Alternative Targets and Therapeutics

The following analysis shows how the number of phenothiazole ring structures and biological targets with quantitative bioactivity data varies depending on the pX activity threshold (Figure 6). Most of the phenothiazines with bioactivity data have a pX value between 5.0 and 5.9. These compounds show activity against 175 targets.

Analysis of phenothiazine structures and associated biological targets | R&D Solutions

Narrowing Focus Further

Examining the data further we can see that 1,174 compounds have biological activity against 250 targets with pX values above 5.0 (Figure 7). Activity against targets such as ataxia telangiectasia mutated protein (ATM), which is a key kinase involved in the DNA damage response-signaling pathway, could provide a new avenue for anticancer research using phenothiazines as the scaffold.

Analysis showing the number of phenothiazine structures | Industry Insights