Table 1.
Binding and second messenger bioassay results
| hMC1R |
hMC3R |
hMC4R |
hMC5R |
|||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| IC50a (nM) | B.E.b (%) | EC50c (nM) | Act. % | IC50 (nM) | B.E. (%) | EC50 (nM) | Act. % | IC50 (nM) | B.E. (%) | EC50 (nM) | Act. % | IC50 (nM) | B.E. (%) | EC50 (nM) | Act. % | |
| HMC001 | 2.2(±0.4) | 80 | >10,000 | 0 | 350(±60) | 70 | >10000 | 0 | >10,000 | — | 2.7 | 30 | >10,000 | — | >10000 | 0 |
| HMC002 | 1.3(±0.3) | 90 | >10,000 | 0 | 5.0(±0.5) | 30 | >10000 | 0 | 1.2(±0.5) | 30 | >10000 | 0 | >10,000 | — | >10000 | 0 |
| HMC009 | >10,000 | — | >10,000 | 0 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 | 0.8 (±0.2) | 50 | >10000 | 0 |
| HMC010 | 4.0(±1.0) | 50 | >10,000 | 0 | 1.2(±0.3) | 50 | >10000 | 0 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 |
| HMC013 | >10,000 | — | >10,000 | 0 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 | 0.5 (±0.1) | 50 | >10000 | 0 |
| HMC014 | >10,000 | — | >10,000 | 0 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 | 0.1(±0.01) | 60 | >10000 | 0 |
| HMC021 | >10,000 | — | >10,000 | 0 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 | 0.4 (±0.1) | 65 | >10000 | 0 |
| HMC025 | >10,000 | — | >10,000 | 20 | >10,000 | — | >10000 | 0 | >10,000 | — | >10000 | 0 | 0.1(±0.01) | 60 | >10000 | 0 |
| MT-II | 0.10(±0.01) | 100 | 1.0(±0.2) | 100 | 1.9(±0.3) | 100 | 2.4(±0.4) | 100 | 1.8(±0.4) | 100 | 2.3(±0.5) | 100 | 7.0(±2.2) | 100 | 8.0(±2.4) | 100 |
a
IC50, concentration of compound at 50% specific binding. Values are means of three experiments done in duplicates; standard deviation is given in parentheses.
b
Binding Efficiency (maximum radioligand displacement by cmpd/maximum radioligand displacement by MT-II).
c
EC50, effective concentration of compound that was able to generate 50% maximal intracellular cAMP accumulation. Compounds were tested at a range of concentrations from 10−10 to 10−5 M.