Table VII.
Functional Activity of N-Me-2 Library at the Mouse Melanocortin Receptors
Ref | mMC1R (nM) | mMC3R (nM) | mMC4R (nM) | mMC5R (nM) |
---|---|---|---|---|
NDP-MSH | 0.0081 ± 0.001 | 0.063 ± 0.004 | 0.097 ± 0.016 | 0.078 ± 0.0084 |
Compound 1 | 64 ± 14 | 770 ± 175 | 4.0 ± 0.6 | 7.0 ± 0.40 |
N-Me-2−1 | 2510 ± 610 | >100,000 | 4900 ± 1800 | 4540 ± 1400 |
N-Me-2−2 | 4100 ± 190 | >100,000 | 2500 ± 330 | 1430 ± 565 |
N-Me-2−4 | 1196 ± 670 | >100,000 | 2877 ± 659 | 2960 ± 995 |
N-Me-2−5 | 1049 ± 312 | >100,000 | 2416 ± 498 | 7990 ± 460 |
N-Me-2−6 | 4900 ± 1030 | >100,000 | 4350 ± 385 | 7010 ± 2900 |
N-Me-2−7 | 8220 ± 7500 | >100,000 | 2710 ± 520 | 3500 ± 1125 |
N-Me-2−8 | 8670 ± 3340 | >100,000 | 860 ± 110 | 900 ± 280 |
N-Me-2−9 | 6167 ± 2687 | >100,000 | 872 ± 379 | 189 ± 28 |
N-Me-2−10 | 8175 ± 1970 | >100,000 | 2493 ± 479 | 2115 ± 392 |
N-Me-2−11 | 6000 ± 4200 | 10,380 ± 2270 | 1050 ± 33 | 1160 ± 365 |
N-Me-2−12 | 8070 ± 2900 | >100,000 | 4900 ± 3200 | 2420 ± 470 |
N-Me-2−13 | 4920 ± 1900 | >100,000 | 1030 ± 109 | 2020 ± 350 |
N-Me-2−14 | 3440 ± 2890 | >100,000 | 498 ± 67 | 740 ± 110 |
N-Me-2−15 | 2478 ± 1566 | >100,000 | 1416 ± 922 | 605 ± 125 |
N-Me-2−16 | 5410 ± 2092 | >100,000 | 1457 ± 731 | 1034 ± 129 |
N-Me-2−17 | 2340 ± 559 | >100,000 | 1552 ± 845 | 1297 ± 100 |
N-Me-2−18 | 8440 ± 4495 | >100,000 | 1850 ± 97 | 4590 ± 930 |