Assay Detail
Binding
CHEMBL843461
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Binding affinity towards mu-opioid receptor by displacement of [3H]NAL at 10 nM from rat brain homogenates
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.57 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317097 | — | — | 1 | 9.59 |
| CHEMBL442195 | — | — | 1 | 8.96 |
| CHEMBL94409 | — | — | 1 | 8.49 |
| CHEMBL264797 | — | — | 1 | 7.64 |
| CHEMBL98403 | — | — | 1 | 7.58 |
| CHEMBL95935 | — | — | 1 | 7.32 |
| CHEMBL439586 | — | — | 1 | 7.30 |
| CHEMBL98407 | — | — | 1 | 7.28 |
| CHEMBL319503 | — | — | 1 | 7.27 |
| CHEMBL95991 | — | — | 1 | 7.20 |
| CHEMBL97779 | — | — | 1 | 7.19 |
| CHEMBL94856 | — | — | 1 | 7.09 |
| CHEMBL97434 | — | — | 1 | 7.08 |
| CHEMBL93614 | — | — | 1 | 7.06 |
| CHEMBL95050 | — | — | 1 | 7.05 |
| CHEMBL98626 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317097 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL442195 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL94409 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL264797 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL98403 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL95935 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL439586 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL98407 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL319503 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL95991 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL97779 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL94856 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL97434 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL93614 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL95050 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL98626 | — | Ki | = | 89.0 | nM | 7.05 |