Assay Detail
Binding
CHEMBL2157129
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Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.43 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.77 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 1 | 6.98 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 6.95 |
| CHEMBL53904 | ZUCLOPENTHIXOL | 3.0 | 1 | 6.77 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 1 | 6.67 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 6.12 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 5.98 |
| CHEMBL46516 | FLUSPIRILENE | 3.0 | 1 | 5.92 |
| CHEMBL2355051 | CLOMIPHENE | 4.0 | 1 | 5.71 |
| CHEMBL1655 | TOREMIFENE | 4.0 | 1 | 5.38 |
| CHEMBL254832 | FENDILINE | 2.0 | 1 | - |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | - |
| CHEMBL25236 | BP-897 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL53904 | ZUCLOPENTHIXOL | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL81 | RALOXIFENE | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 1041.0 | nM | 5.98 |
| CHEMBL46516 | FLUSPIRILENE | Ki | = | 1188.0 | nM | 5.92 |
| CHEMBL2355051 | CLOMIPHENE | Ki | = | 1956.0 | nM | 5.71 |
| CHEMBL1655 | TOREMIFENE | Ki | = | 4125.0 | nM | 5.38 |
| CHEMBL254832 | FENDILINE | Ki | - | — | - | |
| CHEMBL98350 | LY-294002 | Ki | - | — | - | |
| CHEMBL25236 | BP-897 | Ki | - | — | - |