Table 4.
Competitive binding of MSH4, CCK4, 12, 13, 14a–14e, 15a–15d, and 17 to MC4R or CCK2R.
| Compound | MC4R | CCK2R | ||
|---|---|---|---|---|
| Kia (µM) | nb | Kia (nM) | nb | |
| MSH4 | 1.3 ± 0.38 | 5 | ndc | |
| 17 | 1.9 ± 0.14 | 5 | nd | |
| 14a | 7.3 ± 1.1 | 4 | nd | |
| 14b | 1.6 ± 0.16 | 4 | nd | |
| 14c | 0.54 ± 0.04 | 4 | nd | |
| 14d | 0.23 ± 0.02 | 4 | nd | |
| 14e | 0.17 ± 0.02 | 4 | nd | |
| CCK4 | nd | 3.1d | ||
| 12 | nd | 18 ± 5.7 | 3 | |
| 15a | nd | 67 ± 9.4 | 3 | |
| 15b | nd | 1.5 ± 0.7 | 3 | |
| 15c | nd | 2.0 ± 0.3 | 3 | |
| 15d | nd | 0.80 ± 0.2 | 3 | |
| 13 | nbe | 3 | nbe | 2 |
a
Ki values were calculated using the equation Ki = EC50/(1 + ([ligand]/KD)) where [ligand] = 10 nM and KD = 8.3 nM for probe 4 and [ligand] = 2 nM and KD = 34.6 nM for probe 16.
b
The value given represents the average of n independent competition binding experiments, each done in quadruplicate.
c
Not determined.
d
Taken from Reference 30.
e
Compound 13 was unable to inhibit the binding of probe 4 or probe 16 in the concentration range tested (10−5–10−12 M in serine amide).