Assay Detail
Binding
CHEMBL820172
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Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
27
Total Activities
27
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 | 27 | 7.20 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71355 | — | — | 1 | 8.70 |
| CHEMBL306970 | — | — | 1 | 8.15 |
| CHEMBL304060 | — | — | 1 | 8.05 |
| CHEMBL302709 | — | — | 1 | 8.00 |
| CHEMBL70949 | — | — | 1 | 7.72 |
| CHEMBL68085 | — | — | 1 | 7.70 |
| CHEMBL418890 | — | — | 1 | 7.64 |
| CHEMBL71305 | — | — | 1 | 7.58 |
| CHEMBL70981 | — | — | 1 | 7.58 |
| CHEMBL71282 | — | — | 1 | 7.57 |
| CHEMBL73286 | — | — | 1 | 7.51 |
| CHEMBL71797 | — | — | 1 | 7.42 |
| CHEMBL309096 | — | — | 1 | 7.35 |
| CHEMBL442743 | — | — | 1 | 7.25 |
| CHEMBL72945 | — | — | 1 | 7.25 |
| CHEMBL72342 | — | — | 1 | 7.07 |
| CHEMBL302955 | — | — | 1 | 7.03 |
| CHEMBL308741 | — | — | 1 | 7.01 |
| CHEMBL68948 | — | — | 1 | 6.92 |
| CHEMBL307271 | — | — | 1 | 6.82 |
| CHEMBL68033 | — | — | 1 | 6.77 |
| CHEMBL304956 | — | — | 1 | 6.62 |
| CHEMBL303176 | — | — | 1 | 6.57 |
| CHEMBL71712 | — | — | 1 | 6.40 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.39 |
| CHEMBL71283 | — | — | 1 | 5.82 |
| CHEMBL303376 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71355 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL306970 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL304060 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL302709 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL70949 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL68085 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL418890 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL71305 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL70981 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL71282 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL73286 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL71797 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL309096 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL442743 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL72945 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL72342 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL302955 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL308741 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL68948 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL307271 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL68033 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL304956 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL303176 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL71712 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL71283 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL303376 | — | IC50 | = | 2500.0 | nM | 5.60 |