TABLE 2.
Structure-activity relationship of 4-CMTB-based ligands at [35S]GTPγS assay of G protein activation
Values are presented as mean ± S.E.M. Emax is expressed as a percentage of propionate signal. Inactive is defined as <10% propionate maximum signal at the highest concentration tested (10 μM).
| Ligand | FFA2-eYFP |
n | |
|---|---|---|---|
| pEC50 | Emax | ||
| % | |||
| Propionate | 4.39 ± 0.26 | 100.0 ± 4.0 | 3 |
| 4-CMTB | 6.18 ± 0.18 | 105.2 ± 3.8 | 3 |
| S-4-CMTB | 6.52 ± 0.12 | 118.9 ± 5.2 | 3 |
| R-4-CMTB | 5.74 ± 0.09 | 77.7 ± 4.0 | 3 |
| HWD001 | 5.24 ± 0.56 | 69.6 ± 3.0 | 3 |
| HWD002 | 5.50 ± 0.30 | 81.3 ± 3.5 | 3 |
| HWD003 | 5.38 ± 0.13 | 103.4 ± 3.5 | 3 |
| HWD004 | 5.64 ± 0.17 | 90.0 ± 2.6 | 3 |
| HWD005 | 5.50 ± 0.19 | 92.6 ± 3.3 | 3 |
| HWD006 | 5.67 ± 0.38 | 80.1 ± 4.4 | 3 |
| HWD007 | 4.99 ± 0.25 | 88.8 ± 6.0 | 3 |
| HWD008 | 5.04 ± 0.48 | 80.9 ± 9.0 | 3 |
| HWD009 | 5.05 ± 0.30 | 37.1 ± 7.3 | 3 |
| HWD011 | 6.58 ± 0.11 | 128.7 ± 6.4 | 3 |
| HWD012 | Inactive | Inactive | 3 |
| HWD013 | Inactive | Inactive | 3 |
| HWD014 | 5.39 ± 0.26 | 90.0 ± 4.4 | 3 |
| HWD015 | Inactive | Inactive | 3 |
| HWD016 | Inactive | Inactive | 3 |
| HWD017 | 6.11 ± 0.20 | 100.7 ± 3.2 | 3 |
| HWD018 | 4.72 ± 0.33 | 77.5 ± 6.6 | 3 |
| HWD019 | 5.84 ± 0.25 | 96.6 ± 3.4 | 3 |
| S-HWD020 | 5.27 ± 0.16 | 95.2 ± 13.1 | 3 |
| R-HWD020 | Inactive | Inactive | 3 |