Assay Detail
Binding
CHEMBL882499
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Binding affinity against dopamine receptor D2 in rat brain tissue using [3H]spiperone
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.63 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 7.97 |
| CHEMBL285755 | — | — | 1 | 7.27 |
| CHEMBL324750 | — | — | 1 | 7.19 |
| CHEMBL11615 | — | — | 1 | 7.00 |
| CHEMBL301559 | — | — | 1 | 6.47 |
| CHEMBL28437 | — | — | 1 | 6.17 |
| CHEMBL114433 | — | — | 1 | 5.89 |
| CHEMBL28313 | — | — | 1 | 5.87 |
| CHEMBL442203 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273273 | 5-OH-DPAT | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL285755 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL324750 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL11615 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL301559 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL28437 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL114433 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL28313 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL442203 | — | Ki | = | 1570.0 | nM | 5.80 |