Assay Detail
Binding
CHEMBL1780592
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AVP from human vasopressin V1a 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 | 7.04 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779409 | — | — | 1 | 8.00 |
| CHEMBL1779410 | — | — | 1 | 7.89 |
| CHEMBL1779407 | — | — | 1 | 7.82 |
| CHEMBL1779402 | — | — | 1 | 7.31 |
| CHEMBL1779400 | — | — | 1 | 7.26 |
| CHEMBL1779408 | — | — | 1 | 7.13 |
| CHEMBL582857 | NELIVAPTAN | 2.0 | 1 | 7.03 |
| CHEMBL1779406 | — | — | 1 | 7.00 |
| CHEMBL1779404 | — | — | 1 | 6.76 |
| CHEMBL1779417 | — | — | 1 | 6.71 |
| CHEMBL1779401 | — | — | 1 | 6.66 |
| CHEMBL1779420 | — | — | 1 | 6.64 |
| CHEMBL1779419 | — | — | 1 | 6.61 |
| CHEMBL1779418 | — | — | 1 | 6.54 |
| CHEMBL1779403 | — | — | 1 | 6.30 |
| CHEMBL1779405 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779409 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1779410 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1779407 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1779402 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL1779400 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL1779408 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL582857 | NELIVAPTAN | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1779406 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL1779404 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL1779417 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL1779401 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL1779420 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL1779419 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL1779418 | — | Ki | = | 289.0 | nM | 6.54 |
| CHEMBL1779403 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL1779405 | — | Ki | > | 1000.0 | nM | - |