Assay Detail
Binding
CHEMBL818587
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Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 | 32 | 8.16 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543854 | — | — | 1 | 9.05 |
| CHEMBL327242 | — | — | 1 | 8.85 |
| CHEMBL93603 | — | — | 1 | 8.72 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.64 |
| CHEMBL329026 | — | — | 1 | 8.55 |
| CHEMBL328079 | — | — | 1 | 8.55 |
| CHEMBL328791 | — | — | 1 | 8.49 |
| CHEMBL329903 | — | — | 1 | 8.49 |
| CHEMBL432043 | — | — | 1 | 8.43 |
| CHEMBL93861 | — | — | 1 | 8.43 |
| CHEMBL330005 | — | — | 1 | 8.43 |
| CHEMBL539285 | — | — | 1 | 8.43 |
| CHEMBL330016 | — | — | 1 | 8.38 |
| CHEMBL314290 | — | — | 1 | 8.38 |
| CHEMBL327365 | — | — | 1 | 8.30 |
| CHEMBL330094 | — | — | 1 | 8.30 |
| CHEMBL93366 | — | — | 1 | 8.10 |
| CHEMBL92470 | — | — | 1 | 8.05 |
| CHEMBL93195 | — | — | 1 | 8.00 |
| CHEMBL423868 | — | — | 1 | 8.00 |
| CHEMBL93205 | — | — | 1 | 8.00 |
| CHEMBL90657 | — | — | 1 | 7.96 |
| CHEMBL94133 | — | — | 1 | 7.96 |
| CHEMBL329141 | — | — | 1 | 7.89 |
| CHEMBL2093899 | — | — | 1 | 7.82 |
| CHEMBL93209 | — | — | 1 | 7.82 |
| CHEMBL328227 | — | — | 1 | 7.77 |
| CHEMBL92187 | — | — | 1 | 7.75 |
| CHEMBL96731 | — | — | 1 | 7.60 |
| CHEMBL421180 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543854 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL327242 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL93603 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL49429 | LIXIVAPTAN | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL329026 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL328079 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL328791 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL329903 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL432043 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL93861 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL330005 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL539285 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL330016 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL314290 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL330094 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL327365 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL93366 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL92470 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL93195 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL423868 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL93205 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL90657 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL94133 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL329141 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2093899 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL93209 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL328227 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL92187 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL96731 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL421180 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL330494 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL96255 | — | Ki | = | 65.0 | nM | 7.19 |