Assay Detail
Functional
CHEMBL755510
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Incorporation of [35S]GTP-gamma-S, into CHO membranes expressing human Opioid receptor kappa 1
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.27 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 8.96 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 2 | 8.92 |
| CHEMBL169346 | — | — | 2 | 8.55 |
| CHEMBL354172 | — | — | 1 | 8.48 |
| CHEMBL2367916 | — | — | 1 | 8.42 |
| CHEMBL2367604 | — | — | 1 | 8.40 |
| CHEMBL352965 | — | — | 1 | 8.23 |
| CHEMBL422560 | — | — | 1 | 8.01 |
| CHEMBL422563 | — | — | 1 | 8.00 |
| CHEMBL118865 | SPIRADOLINE | 2.0 | 1 | 7.75 |
| CHEMBL2367918 | — | — | 1 | 7.70 |
| CHEMBL2368317 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL56585 | CYCLAZOCINE | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL56585 | CYCLAZOCINE | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL169346 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL354172 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2367916 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2367604 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL169346 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL352965 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL422560 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL422563 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL118865 | SPIRADOLINE | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2367918 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2368317 | — | EC50 | = | 70.0 | nM | 7.16 |