Assay Detail
Binding
CHEMBL2060922
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D₁ receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.75 | 8.90 |
| Ki | 6 | 7.26 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 2 | 9.55 |
| CHEMBL487387 | STEPHOLIDINE | — | 2 | 7.25 |
| CHEMBL2057456 | — | — | 2 | 6.83 |
| CHEMBL2057457 | — | — | 2 | 6.79 |
| CHEMBL2057451 | — | — | 2 | 6.65 |
| CHEMBL2057453 | — | — | 2 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL267930 | SPIPERONE | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL487387 | STEPHOLIDINE | Ki | = | 56.17 | nM | 7.25 |
| CHEMBL487387 | STEPHOLIDINE | IC50 | = | 105.41 | nM | 6.98 |
| CHEMBL2057456 | — | Ki | = | 146.99 | nM | 6.83 |
| CHEMBL2057457 | — | Ki | = | 160.99 | nM | 6.79 |
| CHEMBL2057451 | — | Ki | = | 223.61 | nM | 6.65 |
| CHEMBL2057453 | — | Ki | = | 346.76 | nM | 6.46 |
| CHEMBL2057457 | — | IC50 | = | 456.13 | nM | 6.34 |
| CHEMBL2057456 | — | IC50 | = | 514.46 | nM | 6.29 |
| CHEMBL2057453 | — | IC50 | = | 873.14 | nM | 6.06 |
| CHEMBL2057451 | — | IC50 | = | 1155.3 | nM | 5.94 |