Assay Detail
Binding
CHEMBL841865
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Displacement of [3H]2-BFI (1 nM) from imidazoline receptor I-2 in human brain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 | 6.85 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL147569 | — | — | 1 | 8.19 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.55 |
| CHEMBL146997 | — | — | 1 | 6.90 |
| CHEMBL147044 | — | — | 1 | 6.39 |
| CHEMBL358089 | — | — | 1 | 6.36 |
| CHEMBL147949 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL147569 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL146997 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL147044 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL358089 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL147949 | — | Ki | = | 1920.0 | nM | 5.72 |