Table 1. Summary of competitive binding experiments for compounds evaluated at the mouse melanocortin receptors.
| mMC1R | mMC3R | mMC4R | Selectivity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| IC50 (nM) | IC50 (nM) | IC50 (nM) | Ratios | ||||||||
| Compound Number | Compound Name | Mean ± SEM | n | Fold Diff. | Mean±SEM | n | Fold Diff.* | Mean±SEM | n | Fold Diff. | 1R:3R:4R |
| NDP-MSH | 0.31±0.08 | 6 | 4.18±0.61 | 14 | 1.09±0.12 | 19 | 1:13:4 | ||||
| 1 | 388±52 | 2 | 1 | 60% @100 μM | 2 | 1* | 214±55 | 6 | 1 | 1:374:1 | |
| 2 | CJL-5-35-4 | 178±4 | 2 | 2 | 13400±5100 | 2 | 6 | 83±14 | 4 | 3 | 2:162:1 |
| 3 | CJL-1-116 | 705±6 | 2 | 0.6 | 78% @100 μM | 3 | ND | 292±67 | 4 | 0.7 | 2:ND:1 |
| 4 | CJL-5-35-1 | 225±63 | 2 | 2 | 85% @100 μM | 2 | ND | 841±290 | 2 | 0.3 | 1:ND:4 |
| 5 | CJL-1-41 | 1090±110 | 3 | 0.4 | 8430±230 | 2 | 9 | 258±27 | 2 | 0.8 | 4:33:1 |
| 6 | CJL-1-31 | 27.5±2.2 | 2 | 14 | 3250±760 | 2 | 25 | 33±5.1 | 3 | 6 | 1:119:1 |
| 7 | CJL-1-87 | 68.6±5.3 | 3 | 6 | 3470±510 | 2 | 23 | 9.9±2.9 | 4 | 22 | 7:351:1 |
| 8 | CJL-5-72 | 131±18 | 2 | 3 | 10200±1300 | 2 | 8 | 54±10 | 2 | 4 | 2:190:1 |
|
| |||||||||||
| 9 | 1630±120 | 2 | 1 | 1430±190 | 2 | 1 | 26.0±3.4 | 2 | 1 | 63:55:1 | |
| 10 | CJL-5-35-5 | 997±190 | 2 | 2 | 1310±120 | 2 | 1 | 10.7±0.6 | 2 | 2 | 94:123:1 |
| 11 | CJL-1-132 | 1870±220 | 4 | 1 | 999±290 | 2 | 1 | 21.8±1.9 | 3 | 1 | 85:46:1 |
| 12 | CJL-1-140 | 430±40 | 3 | 4 | 350±80 | 5 | 4 | 10.4±0.03 | 2 | 2 | 41:34:1 |
The experimental compounds were used to displace 125I-NDP-MSH in a dose-response manner to calculate the IC50 values. % represent the amount of 125I-NDP-MSH signal reduction at 100 μM. The “n” column represents the number of independent experiments performed. The reported errors are the standard error of the mean (SEM). ND means not determined.
*
Fold difference for mMC3R was calculated based on an estimated IC50 of 80,000 nM for 1.