Assay Detail
Binding
CHEMBL917731
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells
15
Total Activities
14
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.70 | 8.92 |
| IC50 | 4 | 8.01 | 9.52 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140154 | — | — | 1 | 9.52 |
| CHEMBL339053 | — | — | 2 | 8.92 |
| CHEMBL140738 | — | — | 1 | 8.92 |
| CHEMBL365597 | — | — | 1 | 8.74 |
| CHEMBL360716 | — | — | 1 | 8.19 |
| CHEMBL366706 | — | — | 1 | 7.97 |
| CHEMBL186083 | — | — | 1 | 7.69 |
| CHEMBL390130 | — | — | 1 | 7.36 |
| CHEMBL186841 | — | — | 1 | 7.16 |
| CHEMBL140155 | — | — | 1 | 6.97 |
| CHEMBL143131 | — | — | 1 | 6.62 |
| CHEMBL340355 | — | — | 1 | 6.57 |
| CHEMBL183434 | — | — | 1 | 6.42 |
| CHEMBL424661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140154 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL339053 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL140738 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL365597 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL360716 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL339053 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL366706 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL186083 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL390130 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL186841 | — | Ki | = | 69.5 | nM | 7.16 |
| CHEMBL140155 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL143131 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL340355 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL183434 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL424661 | — | Activity | - | — | - |