Assay Detail
Binding
CHEMBL759232
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Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.63 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290429 | CARFENTANIL | 2.0 | 1 | 10.05 |
| CHEMBL312040 | ETONITAZENE | 2.0 | 1 | 9.30 |
| CHEMBL314209 | — | — | 1 | 9.22 |
| CHEMBL311995 | NALTREXONEDIAZONIUM | — | 1 | 9.22 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.74 |
| CHEMBL310829 | — | — | 1 | 8.70 |
| CHEMBL312046 | — | — | 1 | 8.52 |
| CHEMBL312281 | — | — | 1 | 8.40 |
| CHEMBL81328 | — | — | 1 | 8.10 |
| CHEMBL81465 | — | — | 1 | 7.96 |
| CHEMBL84237 | — | — | 1 | 7.96 |
| CHEMBL309542 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290429 | CARFENTANIL | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL312040 | ETONITAZENE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL314209 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL311995 | NALTREXONEDIAZONIUM | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL19019 | NALTREXONE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL310829 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL312046 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL312281 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL81328 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL81465 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL84237 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL309542 | — | Ki | = | 45.0 | nM | 7.35 |