Assay Detail
Functional
CHEMBL1027276
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
3
Total Activities
2
Compounds Tested
2
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 |
|---|---|---|---|
| Kd | 2 | 8.29 | 8.30 |
| Ki | 1 | 7.72 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL264190 | — | — | 1 | 8.30 |
| CHEMBL454736 | — | — | 2 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL264190 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL454736 | — | Kd | = | 5.248 | nM | 8.28 |
| CHEMBL454736 | — | Ki | = | 19.0 | nM | 7.72 |