Assay Detail
Binding
CHEMBL5046486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-N-methylspiperone from human dopamine D2 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 | 6.06 | 8.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.45 |
| CHEMBL5081136 | — | — | 1 | 8.03 |
| CHEMBL5088070 | — | — | 1 | 7.37 |
| CHEMBL5093200 | — | — | 1 | 7.37 |
| CHEMBL5073754 | — | — | 1 | 7.36 |
| CHEMBL5075726 | — | — | 1 | 7.29 |
| CHEMBL5074399 | — | — | 1 | 7.21 |
| CHEMBL5085974 | — | — | 1 | 7.13 |
| CHEMBL5089655 | — | — | 1 | 6.83 |
| CHEMBL5092243 | — | — | 1 | 6.77 |
| CHEMBL5083441 | — | — | 1 | 6.73 |
| CHEMBL5083473 | — | — | 1 | 6.72 |
| CHEMBL5071238 | — | — | 1 | 6.34 |
| CHEMBL5075990 | — | — | 1 | 6.30 |
| CHEMBL5080654 | — | — | 1 | 6.20 |
| CHEMBL5087543 | — | — | 1 | 6.16 |
| CHEMBL5073904 | — | — | 1 | 6.04 |
| CHEMBL5087504 | — | — | 1 | 6.01 |
| CHEMBL5090215 | — | — | 1 | 5.91 |
| CHEMBL5072449 | — | — | 1 | 5.88 |
| CHEMBL5089932 | — | — | 1 | 5.76 |
| CHEMBL5077104 | — | — | 1 | 5.71 |
| CHEMBL5084145 | — | — | 1 | 5.64 |
| CHEMBL5079053 | — | — | 1 | 5.62 |
| CHEMBL5079903 | — | — | 1 | 5.58 |
| CHEMBL5077114 | — | — | 1 | 5.54 |
| CHEMBL5082465 | — | — | 1 | 5.53 |
| CHEMBL5070377 | — | — | 1 | 5.44 |
| CHEMBL5083186 | — | — | 1 | 5.41 |
| CHEMBL5075014 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.55 | nM | 8.45 |
| CHEMBL5081136 | — | Ki | = | 9.41 | nM | 8.03 |
| CHEMBL5093200 | — | Ki | = | 42.7 | nM | 7.37 |
| CHEMBL5088070 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL5073754 | — | Ki | = | 43.9 | nM | 7.36 |
| CHEMBL5075726 | — | Ki | = | 51.6 | nM | 7.29 |
| CHEMBL5074399 | — | Ki | = | 62.1 | nM | 7.21 |
| CHEMBL5085974 | — | Ki | = | 74.7 | nM | 7.13 |
| CHEMBL5089655 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL5092243 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5083441 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL5083473 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL5071238 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL5075990 | — | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL5080654 | — | Ki | = | 636.0 | nM | 6.20 |
| CHEMBL5087543 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL5073904 | — | Ki | = | 903.0 | nM | 6.04 |
| CHEMBL5087504 | — | Ki | = | 987.0 | nM | 6.01 |
| CHEMBL5090215 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL5072449 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL5089932 | — | Ki | = | 1730.0 | nM | 5.76 |
| CHEMBL5077104 | — | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL5084145 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL5079053 | — | Ki | = | 2380.0 | nM | 5.62 |
| CHEMBL5079903 | — | Ki | = | 2630.0 | nM | 5.58 |
| CHEMBL5077114 | — | Ki | = | 2860.0 | nM | 5.54 |
| CHEMBL5082465 | — | Ki | = | 2950.0 | nM | 5.53 |
| CHEMBL5070377 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL5083186 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL5075014 | — | Ki | = | 4530.0 | nM | 5.34 |
| CHEMBL5086564 | — | Ki | = | 4860.0 | nM | 5.31 |
| CHEMBL5076359 | — | Ki | = | 5240.0 | nM | 5.28 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 5790.0 | nM | 5.24 |
| CHEMBL5077645 | — | Ki | = | 7380.0 | nM | 5.13 |
| CHEMBL5091656 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL346898 | — | Ki | = | 17900.0 | nM | 4.75 |
| CHEMBL5090346 | — | Ki | = | 17600.0 | nM | 4.75 |
| CHEMBL596 | FENTANYL | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL346331 | NORMETHADONE | Ki | = | 34900.0 | nM | 4.46 |
| CHEMBL5087408 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5094044 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5094927 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091479 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091775 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091335 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL651 | METHADONE | Ki | > | 100000.0 | nM | - |