Assay Detail
Binding
CHEMBL882417
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Binding affinity towards Opioid receptor kappa 1 from guinea pig brain using [3H]U-69593 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 | 8.22 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 2 | 10.28 |
| CHEMBL2367604 | — | — | 1 | 10.14 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 3 | 9.77 |
| CHEMBL169536 | — | — | 1 | 9.54 |
| CHEMBL169346 | — | — | 3 | 9.47 |
| CHEMBL422563 | — | — | 1 | 9.30 |
| CHEMBL2367916 | — | — | 3 | 9.27 |
| CHEMBL355403 | — | — | 1 | 9.24 |
| CHEMBL422560 | — | — | 1 | 9.10 |
| CHEMBL354172 | — | — | 1 | 9.00 |
| CHEMBL169345 | — | — | 1 | 9.00 |
| CHEMBL2367918 | — | — | 1 | 8.92 |
| CHEMBL2368318 | — | — | 1 | 8.70 |
| CHEMBL301835 | — | — | 2 | 8.68 |
| CHEMBL352965 | — | — | 1 | 8.66 |
| CHEMBL353303 | — | — | 1 | 8.66 |
| CHEMBL169030 | — | — | 1 | 8.60 |
| CHEMBL168409 | — | — | 1 | 8.54 |
| CHEMBL55851 | — | — | 1 | 8.48 |
| CHEMBL52399 | — | — | 1 | 8.39 |
| CHEMBL168392 | — | — | 1 | 8.24 |
| CHEMBL170384 | — | — | 1 | 8.15 |
| CHEMBL353938 | — | — | 1 | 8.14 |
| CHEMBL2368317 | — | — | 1 | 8.11 |
| CHEMBL291751 | — | — | 1 | 8.07 |
| CHEMBL55392 | — | — | 1 | 8.06 |
| CHEMBL440196 | — | — | 1 | 8.06 |
| CHEMBL422567 | — | — | 1 | 8.04 |
| CHEMBL352365 | — | — | 1 | 8.02 |
| CHEMBL169670 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.052 | nM | 10.28 |
| CHEMBL2367604 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL169536 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL169346 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL422563 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2367916 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL355403 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL422560 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2367916 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL354172 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL169345 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL169346 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2367918 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2368318 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL301835 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL353303 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL352965 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL169030 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL168409 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL55851 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL52399 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL301835 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL168392 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL170384 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL353938 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL2368317 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL291751 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL55392 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL440196 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL422567 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL352365 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL169670 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL56165 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL352827 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL299114 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2367916 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL299114 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL293951 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL168913 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2021605 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL55434 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL169346 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL354322 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL168625 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL55948 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL2368320 | — | Ki | = | 506.0 | nM | 6.30 |