Table 1 BWC0977 is a highly potent and selective inhibitor of bacterial type II topoisomerases

From: Structural interactions of BWC0977 with Klebsiella pneumoniae topoisomerase IV and biochemical basis of its broad-spectrum activity

Compound

IC50 in μM

E. coli gyrase supercoiling

E. coli topo IV decatenation

Human topo IIα decatenation

Human topo IIß decatenation

BWC0977

0.004 ± 0.001

0.013 ± 0.004

113 ± 13

>200

Gepotidacin

0.77 ± 0.2

0.78 ± 0.3

>200

>200

Compound 18c

0.134

0.1634

ND

ND

Ciprofloxacin

0.26 ± 0.02

16 ± 3.1

>200

>200

Levofloxacin

0.39

13

>200

ND

Moxifloxacin

0.29

9.4

>200

ND

Zoliflodacin

0.8

27 ± 12

>200

ND

Teniposide

ND

ND

18 ± 5

92

  1. The compound IC50 values reported for BWC0977, ciprofloxacin and gepotidacin in the table are an average (±standard deviation) of three independent experiments. Compound 18c data is reported from the cited reference. Ciprofloxacin was used as positive reference compound in gyrase and topoisomerase IV assays. Teniposide was used as a positive reference compound in human topoisomerase II decatenation assays.
  2. ND not determined.
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