Assay Detail
Binding
CHEMBL824008
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Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue
34
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.10 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317936 | — | — | 1 | 9.00 |
| CHEMBL98568 | — | — | 2 | 8.72 |
| CHEMBL982 | NALMEFENE | 4.0 | 1 | 8.70 |
| CHEMBL300662 | — | — | 1 | 8.70 |
| CHEMBL97509 | — | — | 1 | 8.64 |
| CHEMBL431266 | — | — | 1 | 8.64 |
| CHEMBL95343 | — | — | 1 | 8.52 |
| CHEMBL98507 | — | — | 2 | 8.48 |
| CHEMBL95647 | — | — | 1 | 8.47 |
| CHEMBL96776 | — | — | 1 | 8.41 |
| CHEMBL329957 | — | — | 1 | 8.32 |
| CHEMBL96058 | — | — | 2 | 8.28 |
| CHEMBL317756 | — | — | 1 | 8.26 |
| CHEMBL97731 | — | — | 1 | 8.24 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.22 |
| CHEMBL319528 | — | — | 1 | 8.19 |
| CHEMBL94577 | — | — | 1 | 8.16 |
| CHEMBL95620 | — | — | 1 | 8.14 |
| CHEMBL97223 | — | — | 1 | 8.02 |
| CHEMBL317097 | — | — | 1 | 8.00 |
| CHEMBL99410 | — | — | 1 | 7.94 |
| CHEMBL330389 | — | — | 1 | 7.93 |
| CHEMBL316760 | — | — | 1 | 7.90 |
| CHEMBL98133 | — | — | 1 | 7.90 |
| CHEMBL97751 | — | — | 1 | 7.84 |
| CHEMBL320218 | — | — | 1 | 7.82 |
| CHEMBL96022 | — | — | 1 | 7.68 |
| CHEMBL97747 | — | — | 1 | 7.54 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.18 |
| CHEMBL328383 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317936 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL98568 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL982 | NALMEFENE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL300662 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL97509 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL431266 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL95343 | — | Ki | = | 3.04 | nM | 8.52 |
| CHEMBL98507 | — | Ki | = | 3.29 | nM | 8.48 |
| CHEMBL95647 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL96776 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL329957 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL96058 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL317756 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL97731 | — | Ki | = | 5.79 | nM | 8.24 |
| CHEMBL98568 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL19019 | NALTREXONE | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL98507 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL319528 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL94577 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL95620 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL97223 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL96058 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL317097 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL99410 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL330389 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL316760 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL98133 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL97751 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL320218 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL96022 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL97747 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL80 | NALOXONE | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL328383 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL318723 | — | Ki | = | 833.0 | nM | 6.08 |