Assay Detail
Binding
CHEMBL900284
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 16 | 7.82 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236521 | — | — | 1 | 9.22 |
| CHEMBL393576 | — | — | 1 | 9.05 |
| CHEMBL393584 | — | — | 1 | 8.60 |
| CHEMBL266647 | — | — | 1 | 8.47 |
| CHEMBL235556 | — | — | 1 | 8.43 |
| CHEMBL236979 | — | — | 1 | 8.22 |
| CHEMBL236731 | — | — | 1 | 8.01 |
| CHEMBL377231 | — | — | 1 | 7.85 |
| CHEMBL211564 | — | — | 1 | 7.72 |
| CHEMBL213122 | — | — | 1 | 7.60 |
| CHEMBL236978 | — | — | 1 | 7.44 |
| CHEMBL236980 | — | — | 1 | 7.41 |
| CHEMBL393583 | — | — | 1 | 7.36 |
| CHEMBL213738 | — | — | 1 | 7.12 |
| CHEMBL236802 | — | — | 1 | 6.58 |
| CHEMBL236804 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236521 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL393576 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL393584 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL266647 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL235556 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL236979 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL236731 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL377231 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL211564 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL213122 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL236978 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL236980 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL393583 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL213738 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL236802 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL236804 | — | Ki | = | 890.0 | nM | 6.05 |