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. 2022 Sep;102(3):172–182. doi: 10.1124/molpharm.122.000549

Fig. 1.

Fig. 1.

In vitro potencies and ADME properties of select analogs of parent compound MBX-2366. (A) Activity in the uptake assay (µM); (B) P. falciparum growth inhibition (µM); (C) cytotoxicity against HeLa cells (µM); (D) solubility in water (µM); (E) murine liver microsome stability (t1/2 in minutes of 1 µM compound in the presence of NADPH at 37°C); (F) Caco-2 permeability, Papp x 10−6 cm/s; (G) stability in the presence of mouse serum (% of compound consumed in 60 minutes); (H) percent protein bound by mouse plasma by equilibrium dialysis; (I) cytochrome P450 3A4 inhibition at 5 µM. NP, not performed.