Assay Detail
Binding
CHEMBL617918
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand
19
Total Activities
19
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 | 19 | 8.04 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.85 |
| CHEMBL64875 | — | — | 1 | 9.48 |
| CHEMBL426763 | — | — | 1 | 9.47 |
| CHEMBL366679 | — | — | 1 | 9.46 |
| CHEMBL367045 | — | — | 1 | 9.19 |
| CHEMBL369367 | — | — | 1 | 9.08 |
| CHEMBL176169 | — | — | 1 | 8.96 |
| CHEMBL368324 | — | — | 1 | 8.83 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL177455 | — | — | 1 | 8.37 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.00 |
| CHEMBL367180 | — | — | 1 | 7.72 |
| CHEMBL362060 | — | — | 1 | 7.70 |
| CHEMBL367087 | — | — | 1 | 7.13 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.79 |
| CHEMBL367875 | — | — | 1 | 6.66 |
| CHEMBL175226 | — | — | 1 | 6.39 |
| CHEMBL177328 | — | — | 1 | 5.70 |
| CHEMBL262794 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL64875 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL426763 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL366679 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL367045 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL369367 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL176169 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL368324 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL715 | OLANZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL177455 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL42 | CLOZAPINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL367180 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL362060 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL367087 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL367875 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL175226 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL177328 | — | Ki | = | 1980.0 | nM | 5.70 |
| CHEMBL262794 | — | Ki | = | 2300.0 | nM | 5.64 |