Assay Detail
Functional
CHEMBL917733
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production
11
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| Intrinsic activity | 9 | - | - |
| Kd | 1 | 7.90 | 7.90 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365597 | — | — | 2 | 7.90 |
| CHEMBL140155 | — | — | 1 | - |
| CHEMBL339053 | — | — | 1 | - |
| CHEMBL340355 | — | — | 1 | - |
| CHEMBL183434 | — | — | 1 | - |
| CHEMBL366706 | — | — | 1 | - |
| CHEMBL360716 | — | — | 1 | - |
| CHEMBL390130 | — | — | 1 | - |
| CHEMBL186083 | — | — | 1 | - |
| CHEMBL186841 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365597 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL365597 | — | Intrinsic activity | = | 3.0 | % | - |
| CHEMBL140155 | — | Activity | - | — | - | |
| CHEMBL339053 | — | Intrinsic activity | = | 100.0 | % | - |
| CHEMBL340355 | — | Intrinsic activity | = | 105.0 | % | - |
| CHEMBL183434 | — | Intrinsic activity | = | 131.0 | % | - |
| CHEMBL366706 | — | Intrinsic activity | = | 105.0 | % | - |
| CHEMBL360716 | — | Intrinsic activity | = | 100.0 | % | - |
| CHEMBL390130 | — | Intrinsic activity | = | 102.0 | % | - |
| CHEMBL186083 | — | Intrinsic activity | = | 14.0 | % | - |
| CHEMBL186841 | — | Intrinsic activity | = | 16.0 | % | - |