Assay Detail
Binding
CHEMBL4828545
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human D2L 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 | 7.81 | 9.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | 2.0 | 1 | 9.93 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 9.16 |
| CHEMBL4865434 | — | — | 1 | 9.16 |
| CHEMBL4846561 | — | — | 1 | 9.02 |
| CHEMBL4873313 | — | — | 1 | 8.75 |
| CHEMBL4853568 | — | — | 1 | 8.73 |
| CHEMBL4847432 | — | — | 1 | 8.72 |
| CHEMBL4861573 | — | — | 1 | 8.65 |
| CHEMBL4850300 | — | — | 1 | 8.64 |
| CHEMBL4860478 | — | — | 1 | 8.60 |
| CHEMBL4864320 | — | — | 1 | 8.59 |
| CHEMBL4856983 | — | — | 1 | 8.14 |
| CHEMBL4868595 | — | — | 1 | 8.13 |
| CHEMBL4849107 | — | — | 1 | 7.60 |
| CHEMBL4853938 | — | — | 1 | 7.56 |
| CHEMBL4871669 | — | — | 1 | 7.42 |
| CHEMBL4858961 | — | — | 1 | 7.18 |
| CHEMBL4876353 | — | — | 1 | 7.13 |
| CHEMBL4864366 | — | — | 1 | 6.79 |
| CHEMBL4871811 | — | — | 1 | 6.76 |
| CHEMBL4858824 | — | — | 1 | 6.69 |
| CHEMBL4875195 | — | — | 1 | 6.66 |
| CHEMBL4862405 | — | — | 1 | 5.88 |
| CHEMBL4869151 | — | — | 1 | 5.75 |
| CHEMBL4868275 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | Ki | = | 0.117 | nM | 9.93 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 0.687 | nM | 9.16 |
| CHEMBL4865434 | — | Ki | = | 0.688 | nM | 9.16 |
| CHEMBL4846561 | — | Ki | = | 0.947 | nM | 9.02 |
| CHEMBL4873313 | — | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL4853568 | — | Ki | = | 1.86 | nM | 8.73 |
| CHEMBL4847432 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4861573 | — | Ki | = | 2.26 | nM | 8.65 |
| CHEMBL4850300 | — | Ki | = | 2.29 | nM | 8.64 |
| CHEMBL4860478 | — | Ki | = | 2.54 | nM | 8.60 |
| CHEMBL4864320 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4856983 | — | Ki | = | 7.24 | nM | 8.14 |
| CHEMBL4868595 | — | Ki | = | 7.42 | nM | 8.13 |
| CHEMBL4849107 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL4853938 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL4871669 | — | Ki | = | 38.2 | nM | 7.42 |
| CHEMBL4858961 | — | Ki | = | 66.4 | nM | 7.18 |
| CHEMBL4876353 | — | Ki | = | 74.4 | nM | 7.13 |
| CHEMBL4864366 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL4871811 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL4858824 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4875195 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL4862405 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL4869151 | — | Ki | = | 1760.0 | nM | 5.75 |
| CHEMBL4868275 | — | Ki | = | 2590.0 | nM | 5.59 |