Assay Detail
Functional
CHEMBL5042988
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Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Characterization of New V<sub>1A</sub> Antagonist Compounds: The Separation of Four Atropisomeric Stereoisomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.18 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799793 | — | — | 1 | 9.00 |
| CHEMBL5070261 | — | — | 1 | 8.96 |
| CHEMBL5074709 | — | — | 1 | 8.92 |
| CHEMBL5070075 | — | — | 1 | 8.74 |
| CHEMBL5081323 | — | — | 1 | 8.72 |
| CHEMBL3416885 | RO-5028442 | 1.0 | 1 | 8.70 |
| CHEMBL4297183 | BALOVAPTAN | 3.0 | 1 | 8.52 |
| CHEMBL1837037 | — | — | 1 | 7.51 |
| CHEMBL5085869 | — | — | 1 | 6.41 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799793 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5070261 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5074709 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5070075 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5081323 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3416885 | RO-5028442 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4297183 | BALOVAPTAN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1837037 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5085869 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL344159 | TOLVAPTAN | IC50 | = | 470.0 | nM | 6.33 |