Assay Detail
Binding
CHEMBL5042987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
20
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Subcellular | Membrane |
| 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 |
|---|---|---|---|
| Ki | 20 | 8.05 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5070261 | — | — | 1 | 9.52 |
| CHEMBL5074709 | — | — | 1 | 9.52 |
| CHEMBL5070075 | — | — | 1 | 9.52 |
| CHEMBL5081323 | — | — | 1 | 9.40 |
| CHEMBL4297183 | BALOVAPTAN | 3.0 | 1 | 9.15 |
| CHEMBL4799793 | — | — | 1 | 9.10 |
| CHEMBL1837037 | — | — | 1 | 8.46 |
| CHEMBL3416885 | RO-5028442 | 1.0 | 1 | 8.26 |
| CHEMBL5078950 | — | — | 2 | 8.20 |
| CHEMBL5088219 | — | — | 1 | 8.06 |
| CHEMBL5071635 | — | — | 2 | 7.96 |
| CHEMBL5074961 | — | — | 1 | 7.92 |
| CHEMBL5079921 | — | — | 2 | 7.52 |
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 7.50 |
| CHEMBL5085869 | — | — | 1 | 7.47 |
| CHEMBL5070501 | — | — | 2 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074709 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5070075 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5070261 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5081323 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4297183 | BALOVAPTAN | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4799793 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1837037 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3416885 | RO-5028442 | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5078950 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5088219 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL5071635 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5074961 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5079921 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL344159 | TOLVAPTAN | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5085869 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL5070501 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL5071635 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL5070501 | — | Ki | = | 999.0 | nM | 6.00 |
| CHEMBL5078950 | — | Ki | = | 2645.0 | nM | 5.58 |
| CHEMBL5079921 | — | Ki | > | 5000.0 | nM | - |