Assay Detail
Binding
CHEMBL617029
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Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand
8
Total Activities
8
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
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.32 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL35057 | TIOSPIRONE | 2.0 | 1 | 9.40 |
| CHEMBL115486 | — | — | 1 | 8.96 |
| CHEMBL114451 | — | — | 1 | 8.69 |
| CHEMBL115367 | — | — | 1 | 8.54 |
| CHEMBL321591 | — | — | 1 | 8.35 |
| CHEMBL326775 | — | — | 1 | 7.99 |
| CHEMBL114131 | — | — | 1 | 7.70 |
| CHEMBL1154 | BENZISOTHIAZOLE-3-YL-PIPERAZINE | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL35057 | TIOSPIRONE | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL115486 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL114451 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL115367 | — | IC50 | = | 2.92 | nM | 8.54 |
| CHEMBL321591 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL326775 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL114131 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL1154 | BENZISOTHIAZOLE-3-YL-PIPERAZINE | IC50 | = | 110.0 | nM | 6.96 |