Table 3. IC50 Values for LasR Inhibition by Library Members in E. coli JLD271 (pJN105L, pSC11)a.
| compound | IC50 (μM)b | 95% CI (μM) | max. inhibition (%)c |
|---|---|---|---|
| 2 (OOHL)d | 0.078 | 0.032–0.19 | 35 |
| 3 (OHHL)d | 10.4 | 5.3–21 | 70 |
| 4e | 2.8 | 1.1–6.8 | 65 |
| 5 | 2.8 | 1.3–6 | 65 |
| 6d | 1.0 | 0.34–3.2 | 70 |
| 7d | 3.5 | 2.6–4.8 | 75 |
| 8d | 0.16 | 0.043–0.57 | 45 |
| 9 | agonist | – | N/A |
| 10 (CL)d | 0.49 | 0.1–2.3 | 40 |
| 11 (ITC-12) | agonist | – | N/A |
| 12 | – | – | N/A |
| 13 | 4.7 | 1.9–12 | 40 |
| 14 | agonist | – | N/A |
| 15 | agonist | – | N/A |
| 16 (mBTL) | agonist | – | N/A |
| 17 (C10-CPA) | – | – | N/A |
| 18 (V-06-018)e | 2.3 | 0.89–6.1 | 50 |
| 19 (TP-1) | agonist | – | N/A |
| 20 (TP-5)e,f | 70 | 56–88 | 85 |
| 21 (C-30)g | – | – | N/A |
| 22 (PD-12) | – | – | N/A |
Antagonism dose–response assays were performed for each compound in the presence of 2 nM OdDHL.
Compounds labeled as “agonist” showed LasR-modulatory activity only at levels ≥100% (the LasR activation level of OdDHL at 2 nM).
Denotes the largest amount of LasR inhibition seen for each compound at any concentration within the dose–response assay. For the full inhibition trace, see Figure S3.