Assay Detail
Binding
CHEMBL617910
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.29 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.85 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 9.64 |
| CHEMBL64875 | — | — | 1 | 9.48 |
| CHEMBL120512 | — | — | 1 | 8.94 |
| CHEMBL368324 | — | — | 1 | 8.83 |
| CHEMBL2111781 | — | — | 1 | 8.76 |
| CHEMBL2111783 | — | — | 2 | 8.46 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL333455 | — | — | 1 | 8.37 |
| CHEMBL332600 | — | — | 1 | 8.29 |
| CHEMBL118889 | — | — | 1 | 8.24 |
| CHEMBL118919 | — | — | 1 | 8.15 |
| CHEMBL119687 | — | — | 1 | 8.06 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.00 |
| CHEMBL121274 | — | — | 1 | 7.92 |
| CHEMBL118092 | — | — | 1 | 7.80 |
| CHEMBL2111782 | — | — | 2 | 7.76 |
| CHEMBL116542 | — | — | 1 | 7.64 |
| CHEMBL333955 | — | — | 1 | 7.64 |
| CHEMBL333246 | — | — | 1 | 7.60 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL64249 | CLOROTEPINE | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL64875 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL120512 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL368324 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL2111781 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL2111783 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL715 | OLANZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2111783 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL333455 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL332600 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL118889 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL118919 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL119687 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL42 | CLOZAPINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL121274 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL118092 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2111782 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL2111782 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL116542 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL333955 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL333246 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 164.0 | nM | 6.79 |