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THPP series potency and properties improvements through structural modification
aavg: average of Papp AB/BA. [r]: ratio.
Comparison of fully active THPP compound BIO-2007817, partially active enantiomer BIO-2007818, and fully inactive compound BIO-198542, all of which are highly soluble and low protein-binding compounds, with moderate permeability. EC50 and Emax were calculated after averaging technical replicates n = 2. See also Figure 3.
