Table 1.
Affinity constants (Ki), effective concentrations (EC50) and efficacy of investigated compounds binding to various PPAR subtypes
| Compound | PPARα | PPARβ/δ | PPARγ | ||
| Ki [μM] | Ki [μM] | Ki [μM] | EC50 [μM] | Efficacy [%] | |
| Amorfrutin 1 | 27 | 27 | 0.236 | 0.458 | 39 |
| Amorfrutin 2 | 25 | 17 | 0.287 | 1.200 | 30 |
| Amorfrutin 3 | 115 | 68 | 0.352 | 4.500 | 22 |
| Amorfrutin 4 | 8 | 6 | 0.278 | 0.979 | 15 |
| Rosiglitazone | n.d. | n.d. | 0.007 | 0.002 | 100 |
| Pioglitazone | n.d. | n.d. | 0.584 | n.d. | n.d. |
| nTZDpa | n.d. | n.d. | 0.029 | n.d. | n.d. |
| Telmisartan | n.d. | n.d. | 1.700 | n.d. | n.d. |
| GW0742 | n.d. | 0.0004 | n.d. | n.d. | n.d. |
| GW7647 | 0.001 | n.d. | 0.180 | n.d. | n.d. |
Ki values were obtained by using a competitive TR-FRET assay, EC50 and efficacy values were determined from a reporter gene assay.
Efficacy is the maximum activation relative to the rosiglitazone-induced activation of PPARs. n.d., not determined