Assay Detail
Functional
CHEMBL1027269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
11
Total Activities
11
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 | 11 | 6.50 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | 9.48 |
| CHEMBL444219 | — | — | 1 | 7.27 |
| CHEMBL491870 | — | — | 1 | 7.07 |
| CHEMBL264190 | — | — | 1 | 6.90 |
| CHEMBL448536 | — | — | 1 | 6.62 |
| CHEMBL503449 | — | — | 1 | 6.28 |
| CHEMBL451423 | — | — | 1 | 6.21 |
| CHEMBL455826 | — | — | 1 | 6.11 |
| CHEMBL510687 | — | — | 1 | 5.91 |
| CHEMBL105113 | — | — | 1 | 4.90 |
| CHEMBL500516 | — | — | 1 | 4.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441738 | AFAMELANOTIDE | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL444219 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL491870 | — | EC50 | = | 84.8 | nM | 7.07 |
| CHEMBL264190 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL448536 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL503449 | — | EC50 | = | 525.0 | nM | 6.28 |
| CHEMBL451423 | — | EC50 | = | 615.0 | nM | 6.21 |
| CHEMBL455826 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL510687 | — | EC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL105113 | — | EC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL500516 | — | EC50 | = | 16400.0 | nM | 4.79 |