Assay Detail
Functional
CHEMBL884503
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Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 5 | 8.02 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140154 | — | — | 1 | 9.22 |
| CHEMBL339053 | — | — | 1 | 8.68 |
| CHEMBL334457 | — | — | 1 | 8.06 |
| CHEMBL140738 | — | — | 1 | 8.02 |
| CHEMBL143131 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140154 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL339053 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL334457 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL140738 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL143131 | — | EC50 | = | 771.0 | nM | 6.11 |