Table 1. Compounds and Their EC50 Obtained Using DMR and Tango Assays, IC50 of SPB05142 To Block the DMR of Each Agonist at Its EC80, and IC50 of Each Agonist To Desensitize the HT-29 Cells Responding to 1μM Zaprinast, and Their Efficacy (That Is, the Maximal Responses) as Measured Using DMR and Tango Assaysa.
| EC50 (μM) |
IC50 (μM) |
efficacy |
||||
|---|---|---|---|---|---|---|
| compd | DMR | Tango | antagonist | desensitization | DMR (pm) | Tango (FRET ratio) |
| Zaprinast | 0.16 ± 0.02 | 6.10 ± 0.45 | 10.5 ± 0.3 | 1.22 ± 0.10 | 269 ± 11 | 12.8 ± 0.1 |
| YE210 | 0.064 ± 0.004 | 17.6 ± 2.3 | 6.90 ± 0.51 | 0.11 ± 0.01 | 283 ± 21 | 13.9 ± 0.1 |
| Luteolin | 7.24 ± 0.51 | 3.20 ± 0.29 | 5.86 ± 0.32 | 18.6 ± 1.2 | 68 ± 5 | 1.5 ± 0.1 |
| Quercetin | 8.02 ± 0.79 | 5.93 ± 0.47 | 6.69 ± 0.51 | 15.4 ± 2.3 | 40 ± 4 | 2.3 ± 0.1 |
| Niflumic acid | 1.15 ± 0.23 | 40.2 ± 3.7 | 14.2 ± 1.5 | 1.28 ± 0.17 | 260 ± 12 | 3.3 ± 0.1 |
| Baicalein | 10.3 ± 1.9 | 22.7 ± 2.1 | 5.02 ± 0.47 | 28.2 ± 1.9 | 248 ± 9 | 2.1 ± 0.1 |
| Myricetin | 3.02 ± 0.37 | 14.7 ± 1.2 | 10.5 ± 1.3 | 2.12 ± 0.20 | 224 ± 11 | 9.2 ± 0.1 |
| Morin | 1.33 ± 0.21 | 11.2 ± 1.3 | 7.42 ± 0.59 | 1.60 ± 0.15 | 284 ± 17 | 9.8 ± 0.1 |
| Lapachol | 2.84 ± 0.35 | 47.9 ± 3.9 | 28.4 ± 2.1 | 4.66 ± 0.36 | 328 ± 22 | 8.7 ± 0.1 |
| Lobaric acid | 2.39 ± 0.42 | 17.6 ± 3.2 | 13.7 ± 1.2 | 4.54 ± 0.39 | 317 ± 21 | 2.0 ± 0.1 |
| Laccacid acid A | 0.39 ± 0.06 | 51.5 ± 6.7 | 11.9 ± 0.9 | 0.39 ± 0.05 | 263 ± 15 | 3.5 ± 0.2 |
| Hematein | 11.1 ± 1.3 | 4.7 ± 1.1 | 3.64 ± 0.41 | 30.4 ± 3.1 | 391 ± 32 | 2.1 ± 0.1 |
| CHCA | 9.80 ± 1.23 | 70.7 ± 6.7 | 8.96 ± 0.71 | 30.4 ± 2.7 | 331 ± 32 | 4.0 ± 0.1 |
| Ellagic acid | 0.11 ± 0.02 | 2.96 ± 0.21 | 2.12 ± 0.19 | 0.10 ± 0.01 | 319 ± 27 | 3.4 ± 0.1 |
| DCA | 0.054 ± 0.004 | 12.4 ± 0.57 | 3.65 ± 0.21 | 0.11 ± 0.01 | 233 ± 12 | 10.9 ± 0.1 |
a
The data represents mean ± s.d. from at least 2 independent measurements (n = 4).