Assay Detail
Functional
CHEMBL900286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.68 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236521 | — | — | 1 | 7.72 |
| CHEMBL393576 | — | — | 1 | 7.68 |
| CHEMBL393584 | — | — | 1 | 7.31 |
| CHEMBL235556 | — | — | 1 | 6.80 |
| CHEMBL213122 | — | — | 1 | 6.24 |
| CHEMBL266647 | — | — | 1 | 6.03 |
| CHEMBL211564 | — | — | 1 | 5.89 |
| CHEMBL377231 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236521 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL393576 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL393584 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL235556 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL213122 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL266647 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL211564 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL377231 | — | IC50 | = | 1700.0 | nM | 5.77 |