Assay Detail
Binding
CHEMBL757327
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Displacement of [3H]nalotrexone from rat-brain Opioid receptors
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.82 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28198 | — | — | 1 | 9.60 |
| CHEMBL12391 | — | — | 1 | 8.89 |
| CHEMBL658 | SUFENTANIL | 4.0 | 1 | 8.64 |
| CHEMBL2304164 | — | — | 1 | 8.60 |
| CHEMBL539579 | — | — | 1 | 8.30 |
| CHEMBL535806 | — | — | 1 | 7.80 |
| CHEMBL556159 | — | — | 1 | 7.77 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 7.60 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.57 |
| CHEMBL174189 | — | — | 1 | 7.16 |
| CHEMBL537622 | — | — | 1 | 6.97 |
| CHEMBL171932 | — | — | 1 | 6.82 |
| CHEMBL172034 | — | — | 1 | 6.00 |
| CHEMBL173897 | — | — | 1 | - |
| CHEMBL556549 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28198 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL12391 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL658 | SUFENTANIL | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2304164 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL539579 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL535806 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL556159 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL596 | FENTANYL | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL70 | MORPHINE | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL174189 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL537622 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL171932 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL172034 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL173897 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL556549 | — | IC50 | > | 1000.0 | nM | - |