Assay Detail
Functional
CHEMBL4199392
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Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of β-Arrestin Biased Ligands of 5-HT7R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.00 | 9.05 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282199 | — | — | 2 | 9.05 |
| CHEMBL4215875 | — | — | 2 | 6.07 |
| CHEMBL4218672 | — | — | 2 | 5.61 |
| CHEMBL4210782 | — | — | 2 | 5.59 |
| CHEMBL4218801 | — | — | 2 | 5.40 |
| CHEMBL4209274 | — | — | 2 | 5.16 |
| CHEMBL4207884 | — | — | 2 | 5.11 |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282199 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL282199 | — | IC50 | = | 0.9333 | nM | 9.03 |
| CHEMBL4215875 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL4215875 | — | IC50 | = | 844.0 | nM | 6.07 |
| CHEMBL4218672 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL4218672 | — | IC50 | = | 2463.0 | nM | 5.61 |
| CHEMBL4210782 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL4210782 | — | IC50 | = | 2556.0 | nM | 5.59 |
| CHEMBL4218801 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4218801 | — | IC50 | = | 3973.0 | nM | 5.40 |
| CHEMBL4209274 | — | IC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL4209274 | — | IC50 | = | 6978.0 | nM | 5.16 |
| CHEMBL4207884 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL4207884 | — | IC50 | = | 7788.0 | nM | 5.11 |
| CHEMBL39 | SEROTONIN | pIC50 | - | — | - | |
| CHEMBL39 | SEROTONIN | IC50 | - | — | - |