Assay Detail
Binding
CHEMBL751572
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Displacement of [3H]DAMGO (2 nM ) from opioid receptor mu 1 in human brain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.55 | 8.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL147044 | — | — | 1 | 8.98 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.54 |
| CHEMBL147949 | — | — | 1 | 7.64 |
| CHEMBL146997 | — | — | 1 | 7.43 |
| CHEMBL358089 | — | — | 1 | 6.36 |
| CHEMBL147569 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL147044 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL596 | FENTANYL | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL147949 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL146997 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL358089 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL147569 | — | Ki | = | 477.0 | nM | 6.32 |