Assay Detail
Binding
CHEMBL5046487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 6.83 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 9.57 |
| CHEMBL5077645 | — | — | 1 | 9.42 |
| CHEMBL5080654 | — | — | 1 | 9.20 |
| CHEMBL5085974 | — | — | 1 | 9.08 |
| CHEMBL5088070 | — | — | 1 | 9.07 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.28 |
| CHEMBL1201294 | DIPHENOXYLATE | 4.0 | 1 | 7.91 |
| CHEMBL651 | METHADONE | 4.0 | 1 | 7.89 |
| CHEMBL5077114 | — | — | 1 | 7.87 |
| CHEMBL5084145 | — | — | 1 | 7.74 |
| CHEMBL5083186 | — | — | 1 | 7.71 |
| CHEMBL5073754 | — | — | 1 | 7.62 |
| CHEMBL346331 | NORMETHADONE | 2.0 | 1 | 7.45 |
| CHEMBL5070377 | — | — | 1 | 7.30 |
| CHEMBL5086564 | — | — | 1 | 7.25 |
| CHEMBL5082465 | — | — | 1 | 7.24 |
| CHEMBL5087543 | — | — | 1 | 7.23 |
| CHEMBL5077104 | — | — | 1 | 7.22 |
| CHEMBL5073904 | — | — | 1 | 7.20 |
| CHEMBL5075726 | — | — | 1 | 7.03 |
| CHEMBL5075990 | — | — | 1 | 6.97 |
| CHEMBL5090215 | — | — | 1 | 6.82 |
| CHEMBL5091335 | — | — | 1 | 6.76 |
| CHEMBL5087504 | — | — | 1 | 6.67 |
| CHEMBL5083473 | — | — | 1 | 6.62 |
| CHEMBL5074399 | — | — | 1 | 6.58 |
| CHEMBL5079903 | — | — | 1 | 6.58 |
| CHEMBL5083441 | — | — | 1 | 6.49 |
| CHEMBL5071238 | — | — | 1 | 6.48 |
| CHEMBL5072449 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | Ki | = | 0.268 | nM | 9.57 |
| CHEMBL5077645 | — | Ki | = | 0.377 | nM | 9.42 |
| CHEMBL5080654 | — | Ki | = | 0.633 | nM | 9.20 |
| CHEMBL5085974 | — | Ki | = | 0.832 | nM | 9.08 |
| CHEMBL5088070 | — | Ki | = | 0.842 | nM | 9.07 |
| CHEMBL596 | FENTANYL | Ki | = | 5.23 | nM | 8.28 |
| CHEMBL1201294 | DIPHENOXYLATE | Ki | = | 12.37 | nM | 7.91 |
| CHEMBL651 | METHADONE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5077114 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL5084145 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL5083186 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL5073754 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL346331 | NORMETHADONE | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL5070377 | — | Ki | = | 50.4 | nM | 7.30 |
| CHEMBL5086564 | — | Ki | = | 56.2 | nM | 7.25 |
| CHEMBL5082465 | — | Ki | = | 57.2 | nM | 7.24 |
| CHEMBL5087543 | — | Ki | = | 58.8 | nM | 7.23 |
| CHEMBL5077104 | — | Ki | = | 60.8 | nM | 7.22 |
| CHEMBL5073904 | — | Ki | = | 63.5 | nM | 7.20 |
| CHEMBL5075726 | — | Ki | = | 92.7 | nM | 7.03 |
| CHEMBL5075990 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL5090215 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL5091335 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL5087504 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL5083473 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL5074399 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL5079903 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL5083441 | — | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL5071238 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL5072449 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL5087408 | — | Ki | = | 474.0 | nM | 6.32 |
| CHEMBL5089655 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL5081136 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL5094044 | — | Ki | = | 649.0 | nM | 6.19 |
| CHEMBL5089932 | — | Ki | = | 866.0 | nM | 6.06 |
| CHEMBL5075014 | — | Ki | = | 988.0 | nM | 6.00 |
| CHEMBL5090346 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL5093200 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2470.0 | nM | 5.61 |
| CHEMBL5091775 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL346898 | — | Ki | = | 3910.0 | nM | 5.41 |
| CHEMBL5092243 | — | Ki | = | 3880.0 | nM | 5.41 |
| CHEMBL5091479 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL5076359 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL5091656 | — | Ki | = | 11100.0 | nM | 4.96 |
| CHEMBL5079053 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL5094927 | — | Ki | = | 15000.0 | nM | 4.82 |