Assay Detail
Binding
CHEMBL751217
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Binding affinity towards Opioid receptor mu 1 from guinea pig brain using [3H]DAMGO as radioligand
52
Total Activities
42
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
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 7.98 | 10.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 2 | 10.49 |
| CHEMBL2367604 | — | — | 1 | 9.77 |
| CHEMBL169536 | — | — | 1 | 9.33 |
| CHEMBL422563 | — | — | 1 | 9.19 |
| CHEMBL301835 | — | — | 2 | 9.17 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 3 | 9.14 |
| CHEMBL355403 | — | — | 1 | 9.04 |
| CHEMBL2367916 | — | — | 3 | 8.96 |
| CHEMBL2367918 | — | — | 1 | 8.74 |
| CHEMBL169345 | — | — | 1 | 8.74 |
| CHEMBL169346 | — | — | 3 | 8.57 |
| CHEMBL2368318 | — | — | 1 | 8.55 |
| CHEMBL169030 | — | — | 1 | 8.52 |
| CHEMBL354172 | — | — | 1 | 8.48 |
| CHEMBL422560 | — | — | 1 | 8.44 |
| CHEMBL422567 | — | — | 1 | 8.38 |
| CHEMBL55851 | — | — | 1 | 8.29 |
| CHEMBL168913 | — | — | 1 | 8.11 |
| CHEMBL168392 | — | — | 1 | 8.08 |
| CHEMBL353303 | — | — | 1 | 8.07 |
| CHEMBL353938 | — | — | 1 | 8.06 |
| CHEMBL56165 | — | — | 1 | 8.05 |
| CHEMBL52399 | — | — | 1 | 8.02 |
| CHEMBL352965 | — | — | 1 | 8.00 |
| CHEMBL291751 | — | — | 1 | 7.89 |
| CHEMBL169670 | — | — | 1 | 7.89 |
| CHEMBL2368317 | — | — | 1 | 7.85 |
| CHEMBL352827 | — | — | 1 | 7.75 |
| CHEMBL168409 | — | — | 1 | 7.75 |
| CHEMBL170384 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2367604 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL169536 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL422563 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL301835 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL355403 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL2367916 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2367916 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL301835 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2367918 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL169345 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL169346 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL2368318 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL169030 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL354172 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL422560 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL422567 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL55851 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL169346 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL168913 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL168392 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL353303 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL353938 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL56165 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL52399 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL352965 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL169670 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL291751 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2368317 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL169346 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL352827 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL170384 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL168409 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL55392 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL352365 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2367916 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL299114 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL293951 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL440196 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL299114 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL168625 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL55434 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2021605 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL354322 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL55248 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL55948 | — | Ki | = | 770.0 | nM | 6.11 |