Assay Detail
Functional
CHEMBL2416144
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Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.20 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2413990 | — | — | 1 | 9.80 |
| CHEMBL2413989 | — | — | 1 | 8.78 |
| CHEMBL2413991 | — | — | 1 | 8.08 |
| CHEMBL211577 | — | — | 1 | 7.97 |
| CHEMBL2413985 | — | — | 1 | 7.61 |
| CHEMBL2413988 | — | — | 1 | 7.52 |
| CHEMBL2413986 | — | — | 1 | 7.32 |
| CHEMBL2413987 | — | — | 1 | 6.82 |
| CHEMBL1043 | DAPSONE | 4.0 | 1 | 6.74 |
| CHEMBL2009408 | — | — | 1 | 6.31 |
| CHEMBL1581846 | — | — | 1 | 6.25 |
| CHEMBL2413984 | — | — | 1 | 6.06 |
| CHEMBL263327 | (PHENYLSULFONYL)BENZENE | — | 1 | 5.80 |
| CHEMBL2413983 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2413990 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL2413989 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL2413991 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL211577 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL2413985 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL2413988 | — | Ki | = | 30.1 | nM | 7.52 |
| CHEMBL2413986 | — | Ki | = | 48.3 | nM | 7.32 |
| CHEMBL2413987 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL1043 | DAPSONE | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL2009408 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL1581846 | — | Ki | = | 564.0 | nM | 6.25 |
| CHEMBL2413984 | — | Ki | = | 866.0 | nM | 6.06 |
| CHEMBL263327 | (PHENYLSULFONYL)BENZENE | Ki | = | 1598.0 | nM | 5.80 |
| CHEMBL2413983 | — | Ki | = | 2039.0 | nM | 5.69 |