Assay Detail
Functional
CHEMBL1027267
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanocyte-stimulating hormone receptor (CHEMBL4077) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.91 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 10.06 |
| CHEMBL491870 | — | — | 1 | 7.42 |
| CHEMBL322610 | — | — | 1 | 7.39 |
| CHEMBL502093 | — | — | 1 | 7.39 |
| CHEMBL444219 | — | — | 1 | 7.27 |
| CHEMBL454736 | — | — | 1 | 7.03 |
| CHEMBL488355 | — | — | 1 | 7.00 |
| CHEMBL264190 | — | — | 1 | 6.95 |
| CHEMBL501394 | — | — | 1 | 6.85 |
| CHEMBL503449 | — | — | 1 | 6.77 |
| CHEMBL455826 | — | — | 1 | 6.75 |
| CHEMBL448536 | — | — | 1 | 6.55 |
| CHEMBL510687 | — | — | 1 | 6.50 |
| CHEMBL501679 | — | — | 1 | 6.27 |
| CHEMBL451423 | — | — | 1 | 5.99 |
| CHEMBL500516 | — | — | 1 | 5.64 |
| CHEMBL105113 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.088 | nM | 10.06 |
| CHEMBL491870 | — | EC50 | = | 38.2 | nM | 7.42 |
| CHEMBL322610 | — | EC50 | = | 40.7 | nM | 7.39 |
| CHEMBL502093 | — | EC50 | = | 40.8 | nM | 7.39 |
| CHEMBL444219 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL454736 | — | EC50 | = | 92.8 | nM | 7.03 |
| CHEMBL488355 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL264190 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL501394 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL503449 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL455826 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL448536 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL510687 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL501679 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL451423 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL500516 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL105113 | — | EC50 | = | 2600.0 | nM | 5.58 |