Assay Detail
Binding
CHEMBL815042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
14
Total Activities
14
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 | 14 | 7.93 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443498 | — | — | 1 | 8.40 |
| CHEMBL104796 | — | — | 1 | 8.40 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.30 |
| CHEMBL430841 | — | — | 1 | 8.30 |
| CHEMBL317673 | — | — | 1 | 8.22 |
| CHEMBL320416 | — | — | 1 | 8.15 |
| CHEMBL105961 | — | — | 1 | 8.00 |
| CHEMBL318392 | — | — | 1 | 7.89 |
| CHEMBL319418 | — | — | 1 | 7.82 |
| CHEMBL318530 | — | — | 1 | 7.72 |
| CHEMBL319433 | — | — | 1 | 7.58 |
| CHEMBL106229 | — | — | 1 | 7.55 |
| CHEMBL321561 | — | — | 1 | 7.52 |
| CHEMBL432009 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443498 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL104796 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL430841 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL317673 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL320416 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL105961 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL318392 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL319418 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL318530 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL319433 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL106229 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL321561 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL432009 | — | IC50 | = | 72.0 | nM | 7.14 |