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. Author manuscript; available in PMC: 2024 Jan 26.
Published in final edited form as: J Med Chem. 2023 Jan 11;66(2):1484–1508. doi: 10.1021/acs.jmedchem.2c01651

Table 4.

N-methylated macrocyclic peptides

ID EC50
(μM)		 β5 IC50 (μM) Permeability Metabolic stability m/hLM Clint Kinet. Solu. Cytotox. cLogP
3D7 Pf20S c-20S i-20S PAMPA Ratio /MDR1
23 graphic file with name nihms-1891577-t0041.jpg 0.21 3.2 >100 >100 186 5.5/37 >768/471 4.2 106 6.0
24 graphic file with name nihms-1891577-t0042.jpg >2.8 >100 >100 >100 283 6.3/23 >768/>768 4 100 6.0
25 graphic file with name nihms-1891577-t0043.jpg 0.25 3.0 >100 >100 339 11/16 >768/>768 <0.85 100 6.3

PAMPA unit: nm/sec at pH7.4; MDR unit: ratio (B→A/A→B); A→B, nm/sec; Metabolic stability Clint unit: μL/min/mg; Kinet. Solu.: Kinetic solubility at pH6.8 (μg/mL); Cytotox.: cytotoxicity, % viability of HepG2 cells at 30 μM. “-”: not tested.