Assay Detail
Functional
CHEMBL899101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.07 | 8.19 |
| Emax | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392760 | — | — | 2 | 8.19 |
| CHEMBL236990 | — | — | 2 | 7.27 |
| CHEMBL363275 | — | — | 2 | 7.14 |
| CHEMBL236987 | — | — | 2 | 7.04 |
| CHEMBL235986 | — | — | 2 | 6.96 |
| CHEMBL235985 | — | — | 2 | 6.83 |
| CHEMBL238277 | — | — | 2 | 6.76 |
| CHEMBL236989 | — | — | 2 | 6.74 |
| CHEMBL394303 | — | — | 2 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392760 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL236990 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL363275 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL236987 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL235986 | — | EC50 | = | 108.5 | nM | 6.96 |
| CHEMBL235985 | — | EC50 | = | 148.0 | nM | 6.83 |
| CHEMBL238277 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL236989 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL394303 | — | EC50 | = | 191.0 | nM | 6.72 |
| CHEMBL363275 | — | Emax | = | 92.0 | % | - |
| CHEMBL392760 | — | Emax | = | 95.5 | % | - |
| CHEMBL236990 | — | Emax | = | 72.0 | % | - |
| CHEMBL236989 | — | Emax | = | 100.0 | % | - |
| CHEMBL394303 | — | Emax | = | 87.5 | % | - |
| CHEMBL238277 | — | Emax | = | 93.5 | % | - |
| CHEMBL235986 | — | Emax | = | 100.0 | % | - |
| CHEMBL235985 | — | Emax | = | 97.5 | % | - |
| CHEMBL236987 | — | Emax | = | 73.0 | % | - |