Assay Detail
Binding
CHEMBL5046489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
46
Total Activities
46
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 | 46 | 5.67 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.85 |
| CHEMBL5083441 | — | — | 1 | 7.72 |
| CHEMBL5089655 | — | — | 1 | 7.59 |
| CHEMBL5083473 | — | — | 1 | 7.42 |
| CHEMBL5092243 | — | — | 1 | 7.20 |
| CHEMBL5088070 | — | — | 1 | 7.19 |
| CHEMBL5085974 | — | — | 1 | 6.99 |
| CHEMBL5073754 | — | — | 1 | 6.42 |
| CHEMBL5087504 | — | — | 1 | 6.38 |
| CHEMBL5073904 | — | — | 1 | 6.37 |
| CHEMBL5093200 | — | — | 1 | 6.33 |
| CHEMBL5074399 | — | — | 1 | 6.30 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 6.26 |
| CHEMBL5081136 | — | — | 1 | 6.17 |
| CHEMBL5071238 | — | — | 1 | 5.90 |
| CHEMBL5075726 | — | — | 1 | 5.80 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 5.73 |
| CHEMBL5087543 | — | — | 1 | 5.56 |
| CHEMBL5075990 | — | — | 1 | 5.47 |
| CHEMBL5072449 | — | — | 1 | 5.42 |
| CHEMBL5077104 | — | — | 1 | 5.41 |
| CHEMBL5080654 | — | — | 1 | 5.26 |
| CHEMBL5075014 | — | — | 1 | 5.25 |
| CHEMBL5089932 | — | — | 1 | 5.18 |
| CHEMBL5079903 | — | — | 1 | 5.07 |
| CHEMBL5070377 | — | — | 1 | 4.90 |
| CHEMBL5082465 | — | — | 1 | 4.86 |
| CHEMBL5090346 | — | — | 1 | 4.86 |
| CHEMBL5084145 | — | — | 1 | 4.75 |
| CHEMBL5086564 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.43 | nM | 8.85 |
| CHEMBL5083441 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL5089655 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL5083473 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL5092243 | — | Ki | = | 63.4 | nM | 7.20 |
| CHEMBL5088070 | — | Ki | = | 64.8 | nM | 7.19 |
| CHEMBL5085974 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL5073754 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL5087504 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL5073904 | — | Ki | = | 426.0 | nM | 6.37 |
| CHEMBL5093200 | — | Ki | = | 466.0 | nM | 6.33 |
| CHEMBL5074399 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL596 | FENTANYL | Ki | = | 554.0 | nM | 6.26 |
| CHEMBL5081136 | — | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL5071238 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL5075726 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL5087543 | — | Ki | = | 2780.0 | nM | 5.56 |
| CHEMBL5075990 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL5072449 | — | Ki | = | 3810.0 | nM | 5.42 |
| CHEMBL5077104 | — | Ki | = | 3930.0 | nM | 5.41 |
| CHEMBL5080654 | — | Ki | = | 5470.0 | nM | 5.26 |
| CHEMBL5075014 | — | Ki | = | 5630.0 | nM | 5.25 |
| CHEMBL5089932 | — | Ki | = | 6610.0 | nM | 5.18 |
| CHEMBL5079903 | — | Ki | = | 8490.0 | nM | 5.07 |
| CHEMBL5070377 | — | Ki | = | 12600.0 | nM | 4.90 |
| CHEMBL5082465 | — | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL5090346 | — | Ki | = | 13900.0 | nM | 4.86 |
| CHEMBL5084145 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL5086564 | — | Ki | = | 17600.0 | nM | 4.75 |
| CHEMBL5094044 | — | Ki | = | 20200.0 | nM | 4.70 |
| CHEMBL346898 | — | Ki | = | 23200.0 | nM | 4.63 |
| CHEMBL5083186 | — | Ki | = | 23400.0 | nM | 4.63 |
| CHEMBL5076359 | — | Ki | = | 26100.0 | nM | 4.58 |
| CHEMBL651 | METHADONE | Ki | = | 26200.0 | nM | 4.58 |
| CHEMBL5077114 | — | Ki | = | 29200.0 | nM | 4.54 |
| CHEMBL5079053 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL5091479 | — | Ki | = | 35400.0 | nM | 4.45 |
| CHEMBL5077645 | — | Ki | = | 36900.0 | nM | 4.43 |
| CHEMBL5090215 | — | Ki | = | 58900.0 | nM | 4.23 |
| CHEMBL346331 | NORMETHADONE | Ki | > | 100000.0 | nM | - |
| CHEMBL5087408 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5094927 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091775 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091335 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091656 | — | Ki | > | 100000.0 | nM | - |