Assay Detail
Binding
CHEMBL942875
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Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.49 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.30 |
| CHEMBL399888 | — | — | 1 | 8.10 |
| CHEMBL400266 | — | — | 1 | 7.85 |
| CHEMBL250346 | — | — | 1 | 7.75 |
| CHEMBL249741 | — | — | 1 | 7.47 |
| CHEMBL400267 | — | — | 1 | 7.36 |
| CHEMBL249340 | — | — | 1 | 7.28 |
| CHEMBL438523 | — | — | 1 | 7.15 |
| CHEMBL399288 | — | — | 1 | 7.12 |
| CHEMBL399289 | — | — | 1 | 7.04 |
| CHEMBL249133 | — | — | 1 | 6.96 |
| CHEMBL251715 | — | — | 1 | - |
| CHEMBL400860 | — | — | 1 | - |
| CHEMBL251561 | — | — | 1 | - |
| CHEMBL249740 | — | — | 1 | - |
| CHEMBL249536 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL399888 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL400266 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL250346 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL249741 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL400267 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL249340 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL438523 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL399288 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL399289 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL249133 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL251715 | — | IC50 | - | — | - | |
| CHEMBL400860 | — | IC50 | - | — | - | |
| CHEMBL251561 | — | IC50 | - | — | - | |
| CHEMBL249740 | — | IC50 | - | — | - | |
| CHEMBL249536 | — | IC50 | > | 200.0 | nM | - |