Assay Detail
Binding
CHEMBL819377
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Inhibition of [3H]AVP binding to recombinant human vasopressin V1a receptor
12
Total Activities
12
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
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.93 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL93366 | — | — | 1 | 7.75 |
| CHEMBL543854 | — | — | 1 | 7.62 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 7.36 |
| CHEMBL327365 | — | — | 1 | 7.31 |
| CHEMBL329903 | — | — | 1 | 7.08 |
| CHEMBL328079 | — | — | 1 | 7.00 |
| CHEMBL328791 | — | — | 1 | 6.96 |
| CHEMBL539285 | — | — | 1 | 6.60 |
| CHEMBL96731 | — | — | 1 | 6.54 |
| CHEMBL330005 | — | — | 1 | 6.39 |
| CHEMBL90657 | — | — | 1 | 6.31 |
| CHEMBL2093899 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL93366 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL543854 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL49429 | LIXIVAPTAN | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL327365 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL329903 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL328079 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL328791 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL539285 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL96731 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL330005 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL90657 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL2093899 | — | Ki | = | 640.0 | nM | 6.19 |