Assay Detail
Functional
CHEMBL3598355
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Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.65 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3596369 | — | — | 1 | 8.23 |
| CHEMBL3596368 | — | — | 1 | 8.17 |
| CHEMBL31421 | — | — | 1 | 8.10 |
| CHEMBL610012 | — | — | 1 | 8.01 |
| CHEMBL3596366 | — | — | 1 | 7.76 |
| CHEMBL3596370 | — | — | 1 | 7.61 |
| CHEMBL3596367 | — | — | 1 | 7.34 |
| CHEMBL47545 | — | — | 1 | 6.94 |
| CHEMBL3596365 | — | — | 1 | 6.66 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | - |
| CHEMBL3596363 | — | — | 1 | - |
| CHEMBL3596364 | — | — | 1 | - |
| CHEMBL3596371 | — | — | 1 | - |
| CHEMBL3596372 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3596369 | — | EC50 | = | 5.85 | nM | 8.23 |
| CHEMBL3596368 | — | EC50 | = | 6.71 | nM | 8.17 |
| CHEMBL31421 | — | EC50 | = | 8.01 | nM | 8.10 |
| CHEMBL610012 | — | EC50 | = | 9.78 | nM | 8.01 |
| CHEMBL3596366 | — | EC50 | = | 17.2 | nM | 7.76 |
| CHEMBL3596370 | — | EC50 | = | 24.7 | nM | 7.61 |
| CHEMBL3596367 | — | EC50 | = | 45.5 | nM | 7.34 |
| CHEMBL47545 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3596365 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL567175 | NALTRINDOLE | EC50 | - | — | - | |
| CHEMBL3596363 | — | EC50 | - | — | - | |
| CHEMBL3596364 | — | EC50 | - | — | - | |
| CHEMBL3596371 | — | EC50 | - | — | - | |
| CHEMBL3596372 | — | EC50 | - | — | - |