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

Table 1. Competitive Binding Assay of Lectin-Targeted Ciprofloxacin Conjugates and Control Compounds with LecA, LecBPAO1, and LecBPA14a.

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LecA
compound n m IC50 ± s.d. [μM]
11 1 LecA-probes 31.7 ± 11
12 2 30.9 ± 8.7
13 3 31.1 ± 8.3
14 4 29.9 ± 9.5
22 1 0 30.4 ± 8.0
23 1 1 21.6 ± 5.5
24 2 0 32.2 ± 3.3
25 2 1 28.0 ± 1.8
26 3 0 27.3 ± 4.0
27 3 1 29.3 ± 3.7
28 4 0 28.3 ± 8.1
29 4 1 26.2 ± 2.4
Me-α-d-Gal controls 71.7 ± 16
pNP-β-d-Gal 52.7 ± 13
  LecBPAO1 LecBPA14
compound m IC50 ± s.d. [μM] IC50 ± s.d. [μM]
19 LecB-probe 3.91 ± 1.6 1.87 ± 0.21
30 0 2.37 ± 1.2 2.24 ± 0.23
31 1 2.53 ± 0.87 1.00 ± 0.06
Me-α-d-Man controls 166 ± 22 101 ± 10
l-Fuc 2.63 ± 1.7 2.46 ± 0.33
Me-α-l-Fuc 0.534 ± 0.07 0.79 ± 0.11
a

Means and standard deviations were determined from a minimum of three independent experiments. Ki calculated from IC50 is shown in Table S1.