Assay Detail
Binding
CHEMBL617656
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Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 14 | 6.99 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 8.54 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.96 |
| CHEMBL70319 | — | — | 1 | 7.89 |
| CHEMBL72794 | — | — | 1 | 7.68 |
| CHEMBL72292 | — | — | 1 | 7.47 |
| CHEMBL308090 | — | — | 1 | 7.09 |
| CHEMBL73074 | — | — | 1 | 7.07 |
| CHEMBL430798 | — | — | 1 | 7.00 |
| CHEMBL73589 | — | — | 1 | 6.55 |
| CHEMBL70377 | — | — | 1 | 6.36 |
| CHEMBL310712 | — | — | 1 | 6.21 |
| CHEMBL307163 | — | — | 1 | 5.92 |
| CHEMBL70609 | — | — | 1 | 5.13 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL70319 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL72794 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL72292 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL308090 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL73074 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL430798 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL73589 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL70377 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL310712 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL307163 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL70609 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL54 | HALOPERIDOL | IC50 | > | 1000.0 | nM | - |