Assay Detail
Functional
CHEMBL4146372
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NG108-15 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.60 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 8.55 |
| CHEMBL4175829 | — | — | 1 | 7.75 |
| CHEMBL4164541 | — | — | 1 | 7.29 |
| CHEMBL4161308 | — | — | 1 | 7.25 |
| CHEMBL4169236 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4175829 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL4164541 | — | IC50 | = | 51.9 | nM | 7.29 |
| CHEMBL4161308 | — | IC50 | = | 56.4 | nM | 7.25 |
| CHEMBL4169236 | — | IC50 | = | 69.5 | nM | 7.16 |