Table V.
Functional Activity of BL3020 Library at the Mouse Melanocortin Receptors
| Refa | 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 1a | 64 ± 14 | 770 ± 175 | 4.0 ± 0.6 | 7.0 ± 0.4 |
| BL3020−4a | 120 ± 28 | 1460 ± 145 | 18 ± 4 | 20 ± 4 |
| BL3020−6 | 590 ± 170 | >100,000 | 29 ± 3 | 51 ± 17 |
| BL3020−7 | 1600 ± 700 | 12,000 ± 2600 | 6.4 ± 1.0 | 73 ± 13 |
| BL3020−8a | 28 ± 12 | 1260 ± 385 | 4 ± 2 | 2 ± 1 |
| BL3020−10 | 740 ± 120 | 11,500 ± 5200 | 3706 ± 4 | 92 ± 6 |
| BL3020−11 | 3300 ± 2200 | >100,000 | 35 ± 6 | 113 ± 15 |
| BL3020−12 | 270 ± 84 | 5530 ± 300 | 17 ± 8 | 25 ± 1 |
| BL3020−13 | 590 ± 77 | 7900 ± 1940 | 9.5 ± 2.0 | 50 ± 14 |
| BL3020−14 | 340 ± 137 | 33 ± 17 | 9.0 ± 0.4 | 16 ± 4 |
| BL3020−15a | 240 ± 41 | 7750 ± 1960 | 5.0 ± 0.1 | 26 ± 17 |
| BL3020−16a | 550 ± 97 | 20,500 ± 2100 | 150 ± 22 | 390 ± 120 |
| BL3020−17 | 28 ± 5 | 840 ± 150 | 1.8 ± 0.1 | 4 ± 1 |
a
Hess et al.11