Assay Detail
Functional
CHEMBL4711048
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Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
2
Total Activities
2
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
A dual-acting 5-HT receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.54 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 7.01 |
| CHEMBL4741978 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4741978 | — | IC50 | = | 860.0 | nM | 6.07 |