Assay Detail
Binding
CHEMBL1780593
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Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.32 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL582857 | NELIVAPTAN | 2.0 | 1 | 6.54 |
| CHEMBL1779400 | — | — | 1 | 6.21 |
| CHEMBL1779404 | — | — | 1 | 6.20 |
| CHEMBL1779401 | — | — | 1 | - |
| CHEMBL1779402 | — | — | 1 | - |
| CHEMBL1779403 | — | — | 1 | - |
| CHEMBL1779405 | — | — | 1 | - |
| CHEMBL1779406 | — | — | 1 | - |
| CHEMBL1779407 | — | — | 1 | - |
| CHEMBL1779408 | — | — | 1 | - |
| CHEMBL1779409 | — | — | 1 | - |
| CHEMBL1779410 | — | — | 1 | - |
| CHEMBL1779417 | — | — | 1 | - |
| CHEMBL1779418 | — | — | 1 | - |
| CHEMBL1779419 | — | — | 1 | - |
| CHEMBL1779420 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL582857 | NELIVAPTAN | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL1779400 | — | Ki | = | 618.0 | nM | 6.21 |
| CHEMBL1779404 | — | Ki | = | 636.0 | nM | 6.20 |
| CHEMBL1779401 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779402 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779403 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779405 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779406 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779407 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779408 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779409 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779410 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779417 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779418 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779419 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1779420 | — | Ki | > | 1000.0 | nM | - |