Assay Detail
Binding
CHEMBL818808
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Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.48 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68085 | — | — | 1 | 8.82 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.64 |
| CHEMBL418890 | — | — | 1 | 8.52 |
| CHEMBL70981 | — | — | 1 | 8.40 |
| CHEMBL71797 | — | — | 1 | 8.40 |
| CHEMBL306970 | — | — | 1 | 8.40 |
| CHEMBL302709 | — | — | 1 | 8.30 |
| CHEMBL71355 | — | — | 1 | 8.15 |
| CHEMBL304956 | — | — | 1 | 7.89 |
| CHEMBL304060 | — | — | 1 | 7.89 |
| CHEMBL73286 | — | — | 1 | 7.85 |
| CHEMBL68948 | — | — | 1 | 7.85 |
| CHEMBL302955 | — | — | 1 | 7.82 |
| CHEMBL71305 | — | — | 1 | 7.66 |
| CHEMBL308741 | — | — | 1 | 7.60 |
| CHEMBL72945 | — | — | 1 | 7.54 |
| CHEMBL71282 | — | — | 1 | 7.54 |
| CHEMBL303176 | — | — | 1 | 7.48 |
| CHEMBL442743 | — | — | 1 | 7.46 |
| CHEMBL70949 | — | — | 1 | 7.38 |
| CHEMBL68033 | — | — | 1 | 7.18 |
| CHEMBL307271 | — | — | 1 | 7.17 |
| CHEMBL309096 | — | — | 1 | 7.11 |
| CHEMBL72342 | — | — | 1 | 6.27 |
| CHEMBL71712 | — | — | 1 | 6.07 |
| CHEMBL303376 | — | — | 1 | 6.07 |
| CHEMBL71283 | — | — | 1 | 5.77 |
| CHEMBL71626 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68085 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL418890 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL70981 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL71797 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL306970 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL302709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL71355 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL304956 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL304060 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL73286 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL68948 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL302955 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL71305 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL308741 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL72945 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL71282 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL303176 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL442743 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL70949 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL68033 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL307271 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL309096 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL72342 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL71712 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL303376 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL71283 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL71626 | — | IC50 | = | 50000.0 | nM | 4.30 |