Table 2.
Competitive binding of NDP-α-MSH, MSH(4), 7, 9a-c, 10a-c, 11, and 12 to hMC4R
| Compounds | IC50 | na |
|---|---|---|
| 7 | nab | 3 |
| 9a | nab | 3 |
| 10a | nab | 3 |
| NDP-α-MSH | 5.9 ± 1.9 nM | 5 |
| 11 | 3.2 ± 0.9 nM | 4 |
| 9b | 3.9 ± 1.2 nM | 5 |
| 10b | 3.3 ± 0.8 nM | 6 |
| MSH(4) | 1.1 ± 0.5 μM | 4 |
| 12 | 0.9 ± 0.1 μM | 4 |
| 9c | 3.3 ± 0.5 μM | 7 |
| 10c | 0.4 ± 0.2 μM | 7 |
a
The IC50 value given is the average of n independent binding experiments, each done in quadruplicate.
b
This compound was unable to displace Eu-NDP-α-MSH in the concentration range tested (10-5-10-12 M).