Assay Detail
Functional
CHEMBL833427
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
23
Total Activities
23
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
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.11 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181066 | — | — | 1 | 9.40 |
| CHEMBL180221 | — | — | 1 | 9.15 |
| CHEMBL444015 | — | — | 1 | 9.10 |
| CHEMBL178385 | — | — | 1 | 8.89 |
| CHEMBL361180 | — | — | 1 | 8.77 |
| CHEMBL180606 | — | — | 1 | 8.57 |
| CHEMBL180066 | — | — | 1 | 8.41 |
| CHEMBL178193 | — | — | 1 | 8.39 |
| CHEMBL178870 | — | — | 1 | 8.07 |
| CHEMBL362487 | — | — | 1 | 8.06 |
| CHEMBL182000 | — | — | 1 | 8.05 |
| CHEMBL359876 | — | — | 1 | 8.03 |
| CHEMBL179277 | — | — | 1 | 8.01 |
| CHEMBL360234 | — | — | 1 | 7.95 |
| CHEMBL444878 | — | — | 1 | 7.86 |
| CHEMBL178234 | — | — | 1 | 7.85 |
| CHEMBL281937 | — | — | 1 | 7.83 |
| CHEMBL180826 | — | — | 1 | 7.71 |
| CHEMBL361572 | — | — | 1 | 7.51 |
| CHEMBL178767 | — | — | 1 | 7.47 |
| CHEMBL180765 | — | — | 1 | 7.37 |
| CHEMBL179592 | — | — | 1 | 7.37 |
| CHEMBL182099 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181066 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL180221 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL444015 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL178385 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL361180 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL180606 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL180066 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL178193 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL178870 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL362487 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL182000 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL359876 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL179277 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL360234 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL444878 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL178234 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL281937 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL180826 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL361572 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL178767 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL180765 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL179592 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL182099 | — | IC50 | = | 169.0 | nM | 6.77 |