Assay Detail
Binding
CHEMBL617605
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Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.10 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 8.22 |
| CHEMBL72794 | — | — | 1 | 7.92 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.92 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.92 |
| CHEMBL70319 | — | — | 1 | 7.64 |
| CHEMBL308090 | — | — | 1 | 7.46 |
| CHEMBL72292 | — | — | 1 | 7.37 |
| CHEMBL430798 | — | — | 1 | 7.32 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.26 |
| CHEMBL73589 | — | — | 1 | 6.96 |
| CHEMBL73074 | — | — | 1 | 6.80 |
| CHEMBL306474 | — | — | 1 | 6.64 |
| CHEMBL70377 | — | — | 1 | 6.51 |
| CHEMBL310712 | — | — | 1 | 6.26 |
| CHEMBL307163 | — | — | 1 | 6.06 |
| CHEMBL70609 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL831 | LOXAPINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL72794 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL70319 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL308090 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL72292 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL430798 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL73589 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL73074 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL306474 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL70377 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL310712 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL307163 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL70609 | — | IC50 | = | 4900.0 | nM | 5.31 |