TABLE 2.
Estimated affinity of ligands at wild type and orthosteric binding pocket mutants of FFA2, competition binding studies using [3H]GLPG0974
The ability of CATPB and GLPG0974 to compete with [3H]GLPG0974 to bind to wild type hFFA2 and each of the indicated mutants of hFFA2 was assessed. Data are presented as calculated affinity constant (pKi) values (mean ± S.E.). ***, p < 0.001. One-way analysis of variance was followed by Dunnett's test with WT as reference.
| Receptor | CATPB | GLPG0974 |
|---|---|---|
| WT | 7.87 ± 0.08 | 7.88 ± 0.08 |
| R255A7.35 | 6.98 ± 0.06*** | 7.59 ± 0.09 |
| R180A5.39 | 7.32 ± 0.06*** | 7.14 ± 0.06*** |
| H242A6.55 | 7.63 ± 0.07 | 8.04 ± 0.04 |
| H140A4.56 | 7.99 ± 0.09 | 8.56 ± 0.10*** |