Assay Detail
Binding
CHEMBL676296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.57 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL369367 | — | — | 1 | 9.60 |
| CHEMBL303313 | — | — | 1 | 9.40 |
| CHEMBL426763 | — | — | 1 | 8.70 |
| CHEMBL366679 | — | — | 1 | 8.57 |
| CHEMBL177455 | — | — | 1 | 8.37 |
| CHEMBL367045 | — | — | 1 | 8.08 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.75 |
| CHEMBL176169 | — | — | 1 | 7.75 |
| CHEMBL64875 | — | — | 1 | 7.68 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.41 |
| CHEMBL367087 | — | — | 1 | 7.18 |
| CHEMBL362060 | — | — | 1 | 6.99 |
| CHEMBL368324 | — | — | 1 | 6.96 |
| CHEMBL367180 | — | — | 1 | 6.95 |
| CHEMBL367875 | — | — | 1 | 6.56 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.50 |
| CHEMBL175226 | — | — | 1 | 6.50 |
| CHEMBL177328 | — | — | 1 | 5.37 |
| CHEMBL262794 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL369367 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL303313 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL426763 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL366679 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL177455 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL367045 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL176169 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL64875 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL715 | OLANZAPINE | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL367087 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL362060 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL368324 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL367180 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL367875 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL42 | CLOZAPINE | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL175226 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL177328 | — | Ki | = | 4255.0 | nM | 5.37 |
| CHEMBL262794 | — | Ki | > | 1000.0 | nM | - |