Table 1. Pharmacologic Properties of Probes 14–17.
| hGPR35 |
|||
|---|---|---|---|
| Compd | EC50a (nM) | IC50b (nM) | IC50c (nM) |
| zaprinast | 0.71 ± 0.12 | — | — |
| 14 | 80.8 ± 9.5 | 9.6 ± 0.7 | 1034.1 ± 95.6 |
| 15 | 49.5 ± 5.6 | 9.4 ± 2.4 | 542.2 ± 87.3 |
| 16 | 42.2 ± 3.3 | 5.6 ± 0.8 | 397.6 ± 65.2 |
| 17 | 58.8 ± 5.8 | 7.8 ± 1.4 | 768.7 ± 84.6 |
a
EC50 to trigger DMR.
b
IC50 to desensitize cells against repeated stimulation of 1 μM zaprinast.
c
IC50 of a known GPR35 antagonist ML-145 to block the agonist-induced DMR. The data represent mean ± SD from two independent measurements, each with four replicates (n = 2).