Assay Detail
Binding
CHEMBL898998
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from dopamine D2 receptor in rat brain
6
Total Activities
6
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 | Intermediate |
Publication
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.67 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.30 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 8.51 |
| CHEMBL136711 | BIRIPERONE | 2.0 | 1 | 7.88 |
| CHEMBL393622 | — | — | 1 | 7.03 |
| CHEMBL393466 | — | — | 1 | 5.65 |
| CHEMBL240733 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL85 | RISPERIDONE | Ki | = | 3.105 | nM | 8.51 |
| CHEMBL136711 | BIRIPERONE | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL393622 | — | Ki | = | 93.76 | nM | 7.03 |
| CHEMBL393466 | — | Ki | = | 2254.24 | nM | 5.65 |
| CHEMBL240733 | — | Ki | < | 100000.0 | nM | - |