Table 3.
Inhibition constants and mechanisms of the best FMNAT hits relative to the FMNAT activity of CaFADS.
| Saturating ATP |
Saturating FMN |
||||
|---|---|---|---|---|---|
| Ki (μM) | Inhibition mechanism | Ki (μM) | K’i (μM) | Inhibition mechanism | |
| 24 | 0.07 ± 0.01 | Non-competitive | 0.08 ± 0.03 | – | Uncompetitive |
| 27 | 0.08 ± 0.01 | Non-competitive | 0.06 ± 0.01 | – | Competitive |
| 31 | 0.09 ± 0.03 | Non-competitive | 3.5 ± 1.0 | 18.4 ± 4.0 | Mixed |
Experimental data recorded at 25 °C in 20 mM PIPES, pH 7.0, 10 mM MgCl2 and 2.5% DMSO. Data obtained by globally fitting the experimental data to the corresponding Lineweawer–Burk inhibition model.