Assay Detail
Functional
CHEMBL715499
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.30 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435368 | — | — | 1 | 7.41 |
| CHEMBL416244 | — | — | 1 | 7.17 |
| CHEMBL40711 | — | — | 1 | 6.80 |
| CHEMBL40233 | — | — | 1 | 6.66 |
| CHEMBL287895 | — | — | 1 | 5.66 |
| CHEMBL40857 | — | — | 1 | 5.57 |
| CHEMBL289532 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435368 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL416244 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL40711 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL40233 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL287895 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL40857 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL289532 | — | Ki | = | 15800.0 | nM | 4.80 |