Assay Detail
Binding
CHEMBL900283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
8
Total Activities
8
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 | 8 | 5.96 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL377231 | — | — | 1 | 6.50 |
| CHEMBL266647 | — | — | 1 | 6.15 |
| CHEMBL393576 | — | — | 1 | 6.12 |
| CHEMBL236521 | — | — | 1 | 6.09 |
| CHEMBL211564 | — | — | 1 | 5.92 |
| CHEMBL213122 | — | — | 1 | 5.89 |
| CHEMBL235556 | — | — | 1 | 5.55 |
| CHEMBL393584 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL377231 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL266647 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL393576 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL236521 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL211564 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL213122 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL235556 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL393584 | — | Ki | = | 3300.0 | nM | 5.48 |