Assay Detail
Functional
CHEMBL1027275
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
16
Total Activities
16
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 | 16 | 7.97 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491870 | — | — | 1 | 9.40 |
| CHEMBL444219 | — | — | 1 | 9.35 |
| CHEMBL502093 | — | — | 1 | 8.97 |
| CHEMBL264190 | — | — | 1 | 8.64 |
| CHEMBL448536 | — | — | 1 | 8.55 |
| CHEMBL501394 | — | — | 1 | 8.47 |
| CHEMBL322610 | — | — | 1 | 8.40 |
| CHEMBL503449 | — | — | 1 | 8.25 |
| CHEMBL510687 | — | — | 1 | 8.06 |
| CHEMBL501679 | — | — | 1 | 7.89 |
| CHEMBL451423 | — | — | 1 | 7.89 |
| CHEMBL455826 | — | — | 1 | 7.20 |
| CHEMBL500516 | — | — | 1 | 6.66 |
| CHEMBL105113 | — | — | 1 | 6.41 |
| CHEMBL488355 | — | — | 1 | 5.36 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491870 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL444219 | — | EC50 | = | 0.45 | nM | 9.35 |
| CHEMBL502093 | — | EC50 | = | 1.07 | nM | 8.97 |
| CHEMBL264190 | — | EC50 | = | 2.28 | nM | 8.64 |
| CHEMBL448536 | — | EC50 | = | 2.84 | nM | 8.55 |
| CHEMBL501394 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL322610 | — | EC50 | = | 3.94 | nM | 8.40 |
| CHEMBL503449 | — | EC50 | = | 5.65 | nM | 8.25 |
| CHEMBL510687 | — | EC50 | = | 8.64 | nM | 8.06 |
| CHEMBL501679 | — | EC50 | = | 12.8 | nM | 7.89 |
| CHEMBL451423 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL455826 | — | EC50 | = | 63.8 | nM | 7.20 |
| CHEMBL500516 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL105113 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL488355 | — | EC50 | = | 4360.0 | nM | 5.36 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.12 | nM | - |