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Binding affinities and potencies of NDP-α-MSH and ACTH analogues at hMC1R, hMC3R and hMC4R.
| hMC1R | hMC3R | hMC4R | ||||
|---|---|---|---|---|---|---|
| Ki(nM) | EC50(nM) | Ki(nM) | EC50(nM) | Ki(nM) | EC50(nM) | |
| NDP-α-MSH | 0.4 ± 0.03 | 0.7 ± 0.1 | 3.5 ± 1.0 | 1.8 ± 0.1 | 2.1 ± 0.2 | 1.0 ± 0.3 |
| NDNal(2’)7-α-MSH | 1.2 ± 0.3 | 1.8 ± 0.5 | 5.5 ± 1.0 | NA | 3.4±0.3 | NA |
| NDPhe7-ACTH1-24 | 0.5 ± 0.2 | 1.0 ± 0.2 | 6.1 ± 0.6 | 0.6 ± 0.1 | 3.9 ± 0.4 | 1.3 ± 0.2 |
| NDNal(2’)7-ACTH1-24 | 0.8 ± 0.3 | 2.7 ± 0.5 | 5.9 ± 0.8 | 83 ± 15 | 3.8 ± 0.1 | 134 ± 32 |
NA: no activity (at 10−6M)
