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. 2022 Aug 22;65(17):11776–11787. doi: 10.1021/acs.jmedchem.2c00791

Table 2. SAR in Pyridine Seriesa.

graphic file with name jm2c00791_0006.jpg

compound T. b. brucei EC50 [nM] T. b. brucei proteasome IC50/human proteasome [nM] LM CLint M/R/H [μL/min/mg] MDCK-MDR1 A to B (ER) [10–6 cm/s]
13 46 17/>10 000 394/114/62 13.5 (0.6)
14 13 19/>10 000 91/48/<25 12.8 (0.6)
15 60   95/43/<25 13.8 (0.7)
a

Details on the biochemical and cellular assay as well as on clearance (Clint) and permeability (MDCK-MDR1) can be found in the Experimental Section.