Assay Detail
Binding
CHEMBL670448
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In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Tissue |
| 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 | 17 | 7.23 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 8.72 |
| CHEMBL426763 | — | — | 1 | 8.72 |
| CHEMBL64875 | — | — | 1 | 8.70 |
| CHEMBL369367 | — | — | 1 | 8.47 |
| CHEMBL177455 | — | — | 1 | 8.23 |
| CHEMBL366679 | — | — | 1 | 8.11 |
| CHEMBL368324 | — | — | 1 | 7.79 |
| CHEMBL367045 | — | — | 1 | 7.71 |
| CHEMBL176169 | — | — | 1 | 7.15 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.07 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.50 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.45 |
| CHEMBL367087 | — | — | 1 | 5.79 |
| CHEMBL367180 | — | — | 1 | 5.76 |
| CHEMBL362060 | — | — | 1 | 5.37 |
| CHEMBL367875 | — | — | 1 | 5.12 |
| CHEMBL175226 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL426763 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL64875 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL369367 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL177455 | — | Ki | = | 5.87 | nM | 8.23 |
| CHEMBL366679 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL368324 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL367045 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL176169 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL715 | OLANZAPINE | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL42 | CLOZAPINE | Ki | = | 353.0 | nM | 6.45 |
| CHEMBL367087 | — | Ki | = | 1621.0 | nM | 5.79 |
| CHEMBL367180 | — | Ki | = | 1741.0 | nM | 5.76 |
| CHEMBL362060 | — | Ki | = | 4285.0 | nM | 5.37 |
| CHEMBL367875 | — | Ki | = | 7604.0 | nM | 5.12 |
| CHEMBL175226 | — | Ki | > | 1000000.0 | nM | - |