Assay Detail
Functional
CHEMBL1019889
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.15 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 9.74 |
| CHEMBL2367604 | — | — | 1 | 9.00 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 8.89 |
| CHEMBL297428 | — | — | 1 | 8.62 |
| CHEMBL33986 | BUTORPHANOL | 4.0 | 1 | 8.54 |
| CHEMBL2107292 | KETAZOCINE | 2.0 | 1 | 8.48 |
| CHEMBL517779 | — | — | 1 | 8.42 |
| CHEMBL464230 | — | — | 1 | 8.36 |
| CHEMBL3275494 | — | — | 1 | 8.09 |
| CHEMBL511691 | — | — | 1 | 8.02 |
| CHEMBL517166 | — | — | 1 | 7.52 |
| CHEMBL290543 | — | — | 1 | 7.44 |
| CHEMBL464071 | — | — | 1 | 7.39 |
| CHEMBL257661 | METAZOCINE | 2.0 | 1 | 6.92 |
| CHEMBL459746 | — | — | 1 | 6.77 |
| CHEMBL511884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511142 | BUPRENORPHINE | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL2367604 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL56585 | CYCLAZOCINE | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL297428 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL33986 | BUTORPHANOL | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2107292 | KETAZOCINE | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL517779 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL464230 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3275494 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL511691 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL517166 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL290543 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL464071 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL257661 | METAZOCINE | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL459746 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL511884 | — | EC50 | - | — | - |