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Table 2 Biological effects of seven potential inhibitors of the YycG histidine kinase

From: Structure-based discovery of inhibitors of the YycG histidine kinase: New chemical leads to combat Staphylococcus epidermidis infections

Chemical inhibitors MICs (μM) a K D value (μM) b IC50 (μM) for YycG' c CC50 (μM) on Vero cell d Hemolysis (%) e
Compound 1 50 27.8 48 >200 < 0.1 (< 0.1)
Compound 2 25 11.1 29 96 2.3 (6.1)
Compound 3 12.5 40.4 15 152 < 0.1 (0.5)
Compound 4 12.5 2.8 13.5 >200 0.1 (0.4)
Compound 5 6.25 2.3 14 >200 0.1 (0.3)
Compound 6 100 -- >200 >200 1.1 (2.3)
Compound 7 0.2 15.7 6.5 >200 < 0.1 (< 0.1)
  1. a The concentrations (μM) listed here were equal to those listed in Table 2, as tested on S. epidermidis ATCC 12228.
  2. b K D value represents the binding affinity of various inhibitors to the YycG' protein, compound 6 showed a very low binding affinity, and could not calculate its K D value with software.
  3. c IC50 represents the concentration of inhibition of 50% the YycG' protein autophosphorylation. As the highest concentration tested was 50 μM, compound 6 displayed poor ability of inhibition.
  4. d CC50 represents the concentration that produce a 50% cytotoxicity effect on Vero cell, as the highest concentration tested corresponding to 200 μM.
  5. e The healthy human erythrocytes were used for the hemolysis assay, and the hemolytic activity of seven inhibitors were shown at their MICs and 4 × MICs (the numbers in the parenthesis) for S. epidermidis ATCC12228 strain.