Assay Detail
Binding
CHEMBL829611
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Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC5R stably expressed in HEK293 cells
6
Total Activities
6
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 | Expert |
Publication
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.12 | 6.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363019 | — | — | 1 | 6.33 |
| CHEMBL188651 | — | — | 1 | 6.32 |
| CHEMBL364560 | — | — | 1 | 6.27 |
| CHEMBL185862 | — | — | 1 | 6.04 |
| CHEMBL365237 | — | — | 1 | 5.92 |
| CHEMBL187659 | — | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363019 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL188651 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL364560 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL185862 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL365237 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL187659 | — | Ki | = | 1400.0 | nM | 5.85 |