Assay Detail
Binding
CHEMBL1019878
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Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 29 | 8.63 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 10.57 |
| CHEMBL297428 | — | — | 1 | 10.22 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 10.15 |
| CHEMBL982 | NALMEFENE | 4.0 | 1 | 9.92 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.72 |
| CHEMBL33986 | BUTORPHANOL | 4.0 | 1 | 9.66 |
| CHEMBL56695 | — | — | 1 | 9.44 |
| CHEMBL415284 | NALORPHINE | 2.0 | 1 | 9.42 |
| CHEMBL517779 | — | — | 1 | 9.41 |
| CHEMBL140278 | — | — | 1 | 9.32 |
| CHEMBL464230 | — | — | 1 | 9.26 |
| CHEMBL468469 | — | — | 1 | 9.25 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 9.21 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.92 |
| CHEMBL3275494 | — | — | 1 | 8.70 |
| CHEMBL517567 | — | — | 1 | 8.68 |
| CHEMBL518083 | — | — | 1 | 8.68 |
| CHEMBL560 | — | — | 1 | 8.52 |
| CHEMBL461227 | — | — | 1 | 8.25 |
| CHEMBL257661 | METAZOCINE | 2.0 | 1 | 8.00 |
| CHEMBL1237044 | TRAMADOL | 4.0 | 1 | 7.85 |
| CHEMBL511884 | — | — | 1 | 7.72 |
| CHEMBL506457 | — | — | 1 | 7.68 |
| CHEMBL442719 | — | — | 1 | 7.52 |
| CHEMBL464250 | — | — | 1 | 7.34 |
| CHEMBL516552 | — | — | 1 | 7.00 |
| CHEMBL511588 | — | — | 1 | 7.00 |
| CHEMBL443601 | — | — | 1 | 6.46 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL297428 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL982 | NALMEFENE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL33986 | BUTORPHANOL | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL56695 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL415284 | NALORPHINE | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL517779 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL140278 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL464230 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL468469 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL80 | NALOXONE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3275494 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL517567 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL518083 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL560 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL461227 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL257661 | METAZOCINE | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL1237044 | TRAMADOL | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL511884 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL506457 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL442719 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL464250 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL516552 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL511588 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL443601 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | Ki | = | 450.0 | nM | 6.35 |