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. 2024 Apr 26;67(9):6987–7005. doi: 10.1021/acs.jmedchem.3c02286

Table 5. Summary of In Vitro ADME Properties of 4, 5, 6, 7, 8, and 1.

  aqueous solubility (μM)
     
compound pH 1.2 pH 6.8 PAMPA permeability (×10–6 cm/s) hepatic microsome stability in rats (mL/min/kg) plasma protein binding in rats (% unbound)
4 <0.02 >100 >50 171 <0.01
5 0.054 >100 >50 237 <0.01
6 <0.01 >100 >50 275 <0.01
7 <0.02 89.5 >50 123 <0.01
8 <0.01 >100 >50 296 <0.01
1a 0.088 >100 >50 38.7 0.51
a

The data are from our previous studies.45,46