TABLE 1.
Summary of binding affinities for FABP1 ligands from DAUDA fluorescence displacement experimentsAll values are reported as means ± S.D. from three replicate experiments conducted on separate days.
| Kd (μM)a | EC50 (μM)b | Fres (% Fluorescence Remaining) | |
|---|---|---|---|
| Arachidonic Acid | 0.08 ± 0.010 | 0.42 ± 0.11 | 2.2 ± 3.6 |
| Diazepam | N.D. | >50 | N.D. |
| Diclofenac | 2.5 ± 1.3 | 3.9 ± 2.1 | 15 ± 3.0 |
| R-Flurbiprofen | N.D. | 4.4 ± 3.8 | 40 ± 1.6 |
| S-Flurbiprofen | 2.2 ± 0.93 | 3.3 ± 1.4 | 48 ± 1.1 |
| Gemfibrozil | 3.6 ± 1.1 | 5.6 ± 1.7 | 18 ± 2.8 |
| Ibuprofen | 9.9 ± 0.60 | 15 ± 0.85 | 28 ± 4.9 |
| Pioglitazone | 1.0 ± 0.30 | 1.8 ± 0.47 | 5.2 ± 2.4 |
| Sulfaphenazole | 15 ± 1.7 | >40 | N.D. |
| Tolbutamide | 20 ± 9.6 | >40 | N.D. |
N.D., not defined, indicates that the parameter could not be determined with confidence.
aKd is the equilibrium binding affinity for the ternary complex formation based on reaction 4 and estimated using numerical simulations conducted in COPASI.
bEC50 is the concentration of ligand at which the fluorescence is decreased by 50% of the maximum decrease observed at residual fluorescence (Fres) value determined from a three-parameter dose response curve fit (eq. 7) to the data obtained from the SVD analysis of the fluorescence titrations.