Assay Detail
Binding
CHEMBL820272
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Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.47 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL320416 | — | — | 1 | 8.40 |
| CHEMBL105961 | — | — | 1 | 8.30 |
| CHEMBL443498 | — | — | 1 | 7.62 |
| CHEMBL430841 | — | — | 1 | 7.62 |
| CHEMBL321561 | — | — | 1 | 7.46 |
| CHEMBL318392 | — | — | 1 | 7.46 |
| CHEMBL432009 | — | — | 1 | 7.23 |
| CHEMBL319433 | — | — | 1 | 7.17 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.82 |
| CHEMBL106229 | — | — | 1 | 6.60 |
| CHEMBL317673 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL320416 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL105961 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL443498 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL430841 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL321561 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL318392 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL432009 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL319433 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL106229 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL317673 | — | IC50 | ~ | 100.0 | nM | - |