Assay Detail
Binding
CHEMBL4828546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure Activity Relationships for a Series of Eticlopride-Based Dopamine D<sub>2</sub>/D<sub>3</sub> Receptor Bitopic Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.29 | 9.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | 2.0 | 1 | 9.97 |
| CHEMBL4865434 | — | — | 1 | 9.55 |
| CHEMBL4861573 | — | — | 1 | 9.37 |
| CHEMBL4873313 | — | — | 1 | 9.36 |
| CHEMBL4864320 | — | — | 1 | 9.35 |
| CHEMBL4850300 | — | — | 1 | 9.31 |
| CHEMBL4846561 | — | — | 1 | 9.30 |
| CHEMBL4860478 | — | — | 1 | 9.10 |
| CHEMBL4847432 | — | — | 1 | 9.09 |
| CHEMBL4856983 | — | — | 1 | 9.00 |
| CHEMBL4853568 | — | — | 1 | 8.96 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.63 |
| CHEMBL4868595 | — | — | 1 | 8.58 |
| CHEMBL4849107 | — | — | 1 | 8.16 |
| CHEMBL4858961 | — | — | 1 | 7.84 |
| CHEMBL4853938 | — | — | 1 | 7.81 |
| CHEMBL4871669 | — | — | 1 | 7.72 |
| CHEMBL4864366 | — | — | 1 | 7.69 |
| CHEMBL4858824 | — | — | 1 | 7.54 |
| CHEMBL4876353 | — | — | 1 | 7.30 |
| CHEMBL4871811 | — | — | 1 | 7.21 |
| CHEMBL4875195 | — | — | 1 | 7.00 |
| CHEMBL4862405 | — | — | 1 | 6.55 |
| CHEMBL4869151 | — | — | 1 | 6.50 |
| CHEMBL4868275 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | Ki | = | 0.107 | nM | 9.97 |
| CHEMBL4865434 | — | Ki | = | 0.281 | nM | 9.55 |
| CHEMBL4861573 | — | Ki | = | 0.431 | nM | 9.37 |
| CHEMBL4873313 | — | Ki | = | 0.436 | nM | 9.36 |
| CHEMBL4864320 | — | Ki | = | 0.444 | nM | 9.35 |
| CHEMBL4850300 | — | Ki | = | 0.493 | nM | 9.31 |
| CHEMBL4846561 | — | Ki | = | 0.499 | nM | 9.30 |
| CHEMBL4860478 | — | Ki | = | 0.797 | nM | 9.10 |
| CHEMBL4847432 | — | Ki | = | 0.815 | nM | 9.09 |
| CHEMBL4856983 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL4853568 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL4868595 | — | Ki | = | 2.63 | nM | 8.58 |
| CHEMBL4849107 | — | Ki | = | 6.97 | nM | 8.16 |
| CHEMBL4858961 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL4853938 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL4871669 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL4864366 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL4858824 | — | Ki | = | 28.7 | nM | 7.54 |
| CHEMBL4876353 | — | Ki | = | 50.3 | nM | 7.30 |
| CHEMBL4871811 | — | Ki | = | 61.1 | nM | 7.21 |
| CHEMBL4875195 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4862405 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL4869151 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL4868275 | — | Ki | = | 426.0 | nM | 6.37 |