Assay Detail
Functional
CHEMBL942878
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Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 21 | 6.81 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249740 | — | — | 1 | 7.96 |
| CHEMBL399888 | — | — | 1 | 7.44 |
| CHEMBL251715 | — | — | 1 | 7.40 |
| CHEMBL249741 | — | — | 1 | 7.28 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 7.04 |
| CHEMBL249340 | — | — | 1 | 7.00 |
| CHEMBL399289 | — | — | 1 | 6.92 |
| CHEMBL249133 | — | — | 1 | 6.85 |
| CHEMBL438523 | — | — | 1 | 6.82 |
| CHEMBL250346 | — | — | 1 | 6.72 |
| CHEMBL400266 | — | — | 1 | 6.44 |
| CHEMBL399288 | — | — | 1 | 6.39 |
| CHEMBL251561 | — | — | 1 | 6.14 |
| CHEMBL400860 | — | — | 1 | 5.98 |
| CHEMBL400267 | — | — | 1 | 5.75 |
| CHEMBL249536 | — | — | 1 | - |
| CHEMBL248929 | — | — | 1 | - |
| CHEMBL248733 | — | — | 1 | - |
| CHEMBL248732 | — | — | 1 | - |
| CHEMBL251771 | — | — | 1 | - |
| CHEMBL400048 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249740 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL399888 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL251715 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL249741 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL249340 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL399289 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL249133 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL438523 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL250346 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL400266 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL399288 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL251561 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL400860 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL400267 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL249536 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL248929 | — | IC50 | - | — | - | |
| CHEMBL248733 | — | IC50 | - | — | - | |
| CHEMBL248732 | — | IC50 | - | — | - | |
| CHEMBL251771 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL400048 | — | IC50 | - | — | - |