Assay Detail
Functional
CHEMBL834452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
20
Total Activities
20
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
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 8.62 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113386 | — | — | 1 | 9.40 |
| CHEMBL609741 | — | — | 1 | 9.10 |
| CHEMBL606639 | — | — | 1 | 9.00 |
| CHEMBL606547 | — | — | 1 | 8.96 |
| CHEMBL609995 | — | — | 1 | 8.96 |
| CHEMBL610254 | — | — | 1 | 8.89 |
| CHEMBL609742 | — | — | 1 | 8.89 |
| CHEMBL609992 | — | — | 1 | 8.89 |
| CHEMBL609737 | — | — | 1 | 8.85 |
| CHEMBL606556 | — | — | 1 | 8.80 |
| CHEMBL606558 | — | — | 1 | 8.66 |
| CHEMBL609994 | — | — | 1 | 8.57 |
| CHEMBL606548 | — | — | 1 | 8.54 |
| CHEMBL606557 | — | — | 1 | 8.49 |
| CHEMBL609993 | — | — | 1 | 8.38 |
| CHEMBL606559 | — | — | 1 | 8.35 |
| CHEMBL609743 | — | — | 1 | 8.35 |
| CHEMBL606705 | — | — | 1 | 8.28 |
| CHEMBL609991 | — | — | 1 | 8.24 |
| CHEMBL606816 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113386 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL609741 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL606639 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL606547 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL609995 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL610254 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL609742 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL609992 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL609737 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL606556 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL606558 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL609994 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL606548 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL606557 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL609993 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL606559 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL609743 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL606705 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL609991 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL606816 | — | EC50 | = | 180.0 | nM | 6.75 |