Assay Detail
Binding
CHEMBL756574
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro affinity to displace [3H]naloxone from opiate receptor in freshly prepared rat brain homogenates
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.02 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL658 | SUFENTANIL | 4.0 | 1 | 10.70 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.67 |
| CHEMBL178035 | — | — | 1 | 8.46 |
| CHEMBL362439 | — | — | 1 | 8.12 |
| CHEMBL367286 | — | — | 1 | 8.09 |
| CHEMBL634 | ALFENTANIL | 4.0 | 1 | 8.09 |
| CHEMBL366899 | — | — | 1 | 8.04 |
| CHEMBL174694 | — | — | 1 | 8.00 |
| CHEMBL367667 | — | — | 1 | 8.00 |
| CHEMBL426034 | — | — | 1 | 7.94 |
| CHEMBL178847 | — | — | 1 | 7.86 |
| CHEMBL176438 | — | — | 1 | 7.86 |
| CHEMBL368487 | — | — | 1 | 7.61 |
| CHEMBL174828 | — | — | 1 | 7.59 |
| CHEMBL174758 | — | — | 1 | 7.57 |
| CHEMBL367661 | — | — | 1 | 7.53 |
| CHEMBL174947 | — | — | 1 | 7.52 |
| CHEMBL367968 | — | — | 1 | 7.39 |
| CHEMBL369412 | — | — | 1 | 7.31 |
| CHEMBL175148 | — | — | 1 | - |
| CHEMBL178434 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL658 | SUFENTANIL | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL596 | FENTANYL | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL178035 | — | Ki | = | 3.49 | nM | 8.46 |
| CHEMBL362439 | — | Ki | = | 7.68 | nM | 8.12 |
| CHEMBL367286 | — | Ki | = | 8.22 | nM | 8.09 |
| CHEMBL634 | ALFENTANIL | Ki | = | 8.21 | nM | 8.09 |
| CHEMBL366899 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL174694 | — | Ki | = | 9.95 | nM | 8.00 |
| CHEMBL367667 | — | Ki | = | 9.95 | nM | 8.00 |
| CHEMBL426034 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL178847 | — | Ki | = | 13.95 | nM | 7.86 |
| CHEMBL176438 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL368487 | — | Ki | = | 24.4 | nM | 7.61 |
| CHEMBL174828 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL174758 | — | Ki | = | 27.14 | nM | 7.57 |
| CHEMBL367661 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL174947 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL367968 | — | Ki | = | 40.5 | nM | 7.39 |
| CHEMBL369412 | — | Ki | = | 49.4 | nM | 7.31 |
| CHEMBL175148 | — | Ki | > | 100.0 | nM | - |
| CHEMBL178434 | — | Ki | > | 100.0 | nM | - |