Assay Detail
Binding
CHEMBL1019876
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Displacement of [3H]DAMGO form human mu 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 | 8.87 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464230 | — | — | 1 | 10.82 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.96 |
| CHEMBL33986 | BUTORPHANOL | 4.0 | 1 | 9.92 |
| CHEMBL517779 | — | — | 1 | 9.82 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 9.80 |
| CHEMBL415284 | NALORPHINE | 2.0 | 1 | 9.72 |
| CHEMBL140278 | — | — | 1 | 9.72 |
| CHEMBL3275494 | — | — | 1 | 9.70 |
| CHEMBL468469 | — | — | 1 | 9.68 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 9.68 |
| CHEMBL297428 | — | — | 1 | 9.51 |
| CHEMBL982 | NALMEFENE | 4.0 | 1 | 9.36 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 9.18 |
| CHEMBL56695 | — | — | 1 | 9.15 |
| CHEMBL517567 | — | — | 1 | 9.11 |
| CHEMBL511884 | — | — | 1 | 8.80 |
| CHEMBL442719 | — | — | 1 | 8.60 |
| CHEMBL518083 | — | — | 1 | 8.59 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.57 |
| CHEMBL257661 | METAZOCINE | 2.0 | 1 | 8.42 |
| CHEMBL464250 | — | — | 1 | 8.35 |
| CHEMBL461227 | — | — | 1 | 8.28 |
| CHEMBL560 | — | — | 1 | 8.16 |
| CHEMBL511588 | — | — | 1 | 8.15 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | 8.07 |
| CHEMBL443601 | — | — | 1 | 8.02 |
| CHEMBL516552 | — | — | 1 | 7.75 |
| CHEMBL506457 | — | — | 1 | 6.40 |
| CHEMBL1237044 | TRAMADOL | 4.0 | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464230 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL33986 | BUTORPHANOL | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL517779 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL415284 | NALORPHINE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL140278 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL3275494 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL468469 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL297428 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL982 | NALMEFENE | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL80 | NALOXONE | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL56695 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL517567 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL511884 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL442719 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL518083 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL257661 | METAZOCINE | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL464250 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL461227 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL560 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL511588 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL443601 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL516552 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL506457 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1237044 | TRAMADOL | Ki | = | 1600.0 | nM | 5.80 |