Assay Detail
Functional
CHEMBL884381
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Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.06 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371292 | — | — | 3 | 7.62 |
| CHEMBL363827 | — | — | 1 | 7.29 |
| CHEMBL371318 | — | — | 1 | 7.23 |
| CHEMBL363843 | — | — | 1 | 7.18 |
| CHEMBL197845 | — | — | 1 | 7.05 |
| CHEMBL196622 | — | — | 1 | 6.99 |
| CHEMBL193824 | — | — | 1 | 6.80 |
| CHEMBL371132 | — | — | 1 | 6.57 |
| CHEMBL194568 | — | — | 1 | 6.46 |
| CHEMBL369910 | — | — | 1 | - |
| CHEMBL193450 | — | — | 1 | - |
| CHEMBL194786 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371292 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL371292 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL363827 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL371318 | — | EC50 | = | 58.5 | nM | 7.23 |
| CHEMBL363843 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL197845 | — | EC50 | = | 89.5 | nM | 7.05 |
| CHEMBL196622 | — | EC50 | = | 102.8 | nM | 6.99 |
| CHEMBL193824 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL371132 | — | EC50 | = | 269.5 | nM | 6.57 |
| CHEMBL194568 | — | EC50 | = | 344.5 | nM | 6.46 |
| CHEMBL371292 | — | EC50 | = | - | nM | - |
| CHEMBL369910 | — | EC50 | = | - | nM | - |
| CHEMBL193450 | — | EC50 | = | - | nM | - |
| CHEMBL194786 | — | EC50 | = | - | nM | - |