Table 2. Potencies and Binding Affinities of the Selected GPR35 Ligands.
| Compd | BRET assay Ki (μM)a | Reference Ki (μM)b | DMR assay (μM)c | β-arrestin assay (μM)d |
|---|---|---|---|---|
| 18 | 2.97 ± 0.87 | 2.340 ± 0.040 | (EC50) 0.5222 | (EC50) 722 |
| 19 | 0.612 ± 0.233 | 0.401 ± 0.015 | (EC50) 0.1623 | (EC50) 4.223 |
| 20 | 0.023 ± 0.006 | 0.012 ± 0.001 | (EC50) 0.00324 | (EC50) 1.20 ± 0.1325 |
| 21 | 0.004 ± 0.001 | 0.009 ± 0.001 | / | (IC50) 0.02725 |
| 22 | 0.236 ± 0.049 | 0.042 ± 0.003 | (IC50) 10.423 | (IC50) 0.2025 |
| 23 | 0.332 ± 0.063 | / | (EC50) 0.071 ± 0.01012 | / |
| 24 | 0.051 ± 0.015 | / | (EC50) 0.006 ± 0.00126 | (EC50) 0.197 ± 0.03823 |
| 25 | 0.010 ± 0.002 | / | (EC50) 0.059 ± 0.00728 | / |
| 26 | 0.352 ± 0.107 | / | (EC50) 0.150 ± 0.02026 | (EC50) 3.63 ± 0.9523 |
| 27 | 0.028 ± 0.006 | / | (EC50) 0.083 ± 0.00612 | / |
| 28 (DQDA) | 0.006 ± 0.002 | / | (EC50) 0.008 ± 0.00112 | / |
a
Affinities were determined through displacement BRET binding assays using 25 nM 15. The data represent mean ± SD from three independent measurements, each with three replicates (n = 3).
b
Ki values were acquired from radio–ligand binding assays from the literature.9 /: not measured or reported.
c
EC50 values were tested by DMR assays in HT-29 cells endogenously expressing GPR35.
d
Previously published. /: not measured or reported.