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. 2015 Oct 22;137(46):14626–14639. doi: 10.1021/jacs.5b06728

Table 5. Comparison of LasR Antagonist or Agonist Potency between Pump-Active (PAO-JP2) and Pump-Mutant (PAO-JG21) P. aeruginosa LasR Reporter Strainsa.

antagonism
compoundb PAO-JP2 IC50 (μM) PAO-JG21 IC50 (μM) fold changec
2 (OOHL) 5.5 0.57 9.6
3 (OHHL) 40 41 1.0
5 73 8.9 8.2
6 175 20 8.8
7 116 8.2 14.1
8 12 1.5 8.0
9 3 0.42 7.1
10 (CL) 21 1.3 16.2
12 9.7 3.7 2.6
18 (V-06-018) 5.2 6.1 0.9
20 (TP-5) 69 63 1.1
22 (PD-12) 2.5 0.11 22.7
agonism
compound PAO-JP2 IC50 (μM) PAO-JG21 IC50 (μM) fold changeb
1 (OdDHL) 0.14 0.019 7.4
2 >200 26 >7.7
8 >200 24 >8.3
9 140 8.6 16.3
11 (ITC-12) 2.6 1.3 2.0
14 17 15 1.1
16 (mBTL) 4.2 0.56 7.5
19 (TP-1) 0.071 0.036 2.0
a

Both strains utilize the plasmid plasI-LVAgfp to report compound ability to mediate LasR expression of lasI-LVAgfp.

b

Data for compounds with incalculable fold-changes in potency (due to incomplete dose–response curves) are listed in Table S4.

c

Compounds with statistically insignificant shifts in EC50 (p > 0.1) are shown in bold. For statistical analysis, see Table S4.