Assay Detail
Binding
CHEMBL1787311
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Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | tsA201 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.34 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.00 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 7.89 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.85 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.82 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.66 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 7.48 |
| CHEMBL1782360 | — | — | 1 | 7.39 |
| CHEMBL1782363 | — | — | 1 | 7.31 |
| CHEMBL1782357 | — | — | 1 | 7.31 |
| CHEMBL1782362 | — | — | 1 | 7.24 |
| CHEMBL1782364 | — | — | 1 | 7.21 |
| CHEMBL1782359 | — | — | 1 | 7.17 |
| CHEMBL1782356 | — | — | 1 | 7.13 |
| CHEMBL1782358 | — | — | 1 | 7.11 |
| CHEMBL1782365 | — | — | 1 | 7.08 |
| CHEMBL1782355 | — | — | 1 | 7.04 |
| CHEMBL1782361 | — | — | 1 | 6.92 |
| CHEMBL211688 | — | — | 1 | 6.82 |
| CHEMBL1782366 | — | — | 1 | 6.75 |
| CHEMBL1782367 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL715 | OLANZAPINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL42 | CLOZAPINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL85 | RISPERIDONE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL1782360 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1782363 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL1782357 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL1782362 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL1782364 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1782359 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1782356 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL1782358 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL1782365 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL1782355 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL1782361 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL211688 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1782366 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1782367 | — | Ki | = | 280.0 | nM | 6.55 |