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. 2020 Sep 14;63(20):11707–11724. doi: 10.1021/acs.jmedchem.0c00856

Table 3. Early ADMET Data on Two Representative Lectin-Targeted Conjugates (22 and 30) and Ciprofloxacin (3): All Compounds Were Metabolically Stable in Human Plasma and Microsomal Fractions. Cytotoxicity was reduced compared to ciprofloxacina.

  metabolic stability
   
  t1/2 [min] CLMIC [μL/min/mg protein]
plasma protein binding [%] cytotoxicity @ 100 μM [% inhibition]
compound human plasma MLM HLM human plasma HEK293 A549
22 >150 10 10 69 ± 7 8 ± 4 5 ± 22
30 >150 10 15 75 ± 10 11 ± 12 –9 ± 15
3 >150 n.d. n.d. 33 ± 2 48 ± 5 18 ± 11
a

Data is presented as mean and standard deviation from at least two independent experiments (exception: one experiment for CLMIC data). MLM, mouse liver microsomes; HLM, human liver microsomes; n.d., not determined.