Assay Detail
Binding
CHEMBL759238
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Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.03 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.97 |
| CHEMBL345120 | — | — | 1 | 8.72 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.67 |
| CHEMBL162700 | — | — | 1 | 8.58 |
| CHEMBL347188 | — | — | 1 | 8.39 |
| CHEMBL161084 | MIRFENTANIL | 2.0 | 1 | 8.12 |
| CHEMBL157922 | — | — | 1 | 8.11 |
| CHEMBL158857 | — | — | 1 | 7.86 |
| CHEMBL161021 | — | — | 1 | 7.81 |
| CHEMBL161023 | — | — | 1 | 7.73 |
| CHEMBL161147 | — | — | 1 | 7.67 |
| CHEMBL161082 | — | — | 1 | 7.65 |
| CHEMBL158856 | — | — | 1 | 7.45 |
| CHEMBL161280 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80 | NALOXONE | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL345120 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL596 | FENTANYL | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL162700 | — | Ki | = | 2.64 | nM | 8.58 |
| CHEMBL347188 | — | Ki | = | 4.05 | nM | 8.39 |
| CHEMBL161084 | MIRFENTANIL | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL157922 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL158857 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL161021 | — | Ki | = | 15.6 | nM | 7.81 |
| CHEMBL161023 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL161147 | — | Ki | = | 21.3 | nM | 7.67 |
| CHEMBL161082 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL158856 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL161280 | — | Ki | = | 214.0 | nM | 6.67 |