Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| A-375 | EC50 | 110 nM | Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | [PMID: 26218460] |
| A-375 | IC50 | 6.7 nM | Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | [PMID: 26218460] |
| HEK293 | EC50 | 0.021 nM | Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay | [PMID: 15615519] |
| HEK293 | EC50 | 0.03 nM | Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | [PMID: 25347033] |
| HEK293 | EC50 | 0.04 nM | Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay | [PMID: 15615519] |
| HEK293 | EC50 | 0.05 nM | Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | [PMID: 25699138] |
| HEK293 | EC50 | 0.06 nM | Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | [PMID: 25347033] |
| HEK293 | EC50 | 0.17 nM | Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay | [PMID: 15615519] |
| HEK293 | EC50 | 0.18 nM | Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | [PMID: 25347033] |
| HEK293 | EC50 | 0.18 nM | Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay | [PMID: 15615519] |
| HEK293 | EC50 | 0.19 nM | Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | [PMID: 25347033] |
| HEK293 | EC50 | 0.22 nM | Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | [PMID: 25699138] |
| HEK293 | EC50 | 0.3 nM | Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation | [PMID: 16539382] |
| HEK293 | EC50 | 0.35 nM | Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | [PMID: 25699138] |
| HEK293 | EC50 | 0.57 nM | Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | [PMID: 25699138] |
| HEK293 | IC50 | 1 nM | Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis | [PMID: 25699148] |
| HEK293 | EC50 | 1 nM | Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | [PMID: 16931008] |
| HEK293 | EC50 | 1.02 nM | Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | [PMID: 25699148] |
| HEK293 | IC50 | 1.1 nM | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | [PMID: 26599352] |
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