Assay Detail
Functional
CHEMBL1027278
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC5R 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 |
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 | 7.93 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.59 |
| CHEMBL491870 | — | — | 1 | 8.83 |
| CHEMBL444219 | — | — | 1 | 8.69 |
| CHEMBL502093 | — | — | 1 | 8.59 |
| CHEMBL448536 | — | — | 1 | 8.54 |
| CHEMBL264190 | — | — | 1 | 8.49 |
| CHEMBL503449 | — | — | 1 | 8.28 |
| CHEMBL501394 | — | — | 1 | 8.13 |
| CHEMBL322610 | — | — | 1 | 8.13 |
| CHEMBL501679 | — | — | 1 | 8.10 |
| CHEMBL451423 | — | — | 1 | 7.75 |
| CHEMBL454736 | — | — | 1 | 7.65 |
| CHEMBL510687 | — | — | 1 | 7.52 |
| CHEMBL455826 | — | — | 1 | 7.29 |
| CHEMBL500516 | — | — | 1 | 6.65 |
| CHEMBL488355 | — | — | 1 | 6.47 |
| CHEMBL105113 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL491870 | — | EC50 | = | 1.47 | nM | 8.83 |
| CHEMBL444219 | — | EC50 | = | 2.04 | nM | 8.69 |
| CHEMBL502093 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL448536 | — | EC50 | = | 2.85 | nM | 8.54 |
| CHEMBL264190 | — | EC50 | = | 3.26 | nM | 8.49 |
| CHEMBL503449 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL501394 | — | EC50 | = | 7.42 | nM | 8.13 |
| CHEMBL322610 | — | EC50 | = | 7.41 | nM | 8.13 |
| CHEMBL501679 | — | EC50 | = | 8.03 | nM | 8.10 |
| CHEMBL451423 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL454736 | — | EC50 | = | 22.4 | nM | 7.65 |
| CHEMBL510687 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL455826 | — | EC50 | = | 51.1 | nM | 7.29 |
| CHEMBL500516 | — | EC50 | = | 226.0 | nM | 6.65 |
| CHEMBL488355 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL105113 | — | EC50 | = | 730.0 | nM | 6.14 |