Assay Detail
Binding
CHEMBL712747
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Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.83 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140154 | — | — | 1 | 9.52 |
| CHEMBL334457 | — | — | 1 | 9.30 |
| CHEMBL339053 | — | — | 1 | 8.92 |
| CHEMBL140738 | — | — | 1 | 8.92 |
| CHEMBL140155 | — | — | 1 | 6.97 |
| CHEMBL140108 | — | — | 1 | 6.90 |
| CHEMBL143131 | — | — | 1 | 6.62 |
| CHEMBL342954 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140154 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL334457 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL339053 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL140738 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL140155 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL140108 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL143131 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL342954 | — | IC50 | = | 3050.0 | nM | 5.52 |