Assay Detail
Binding
CHEMBL5148372
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Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzodiazepine Derivatives as Potent Vasopressin V<sub>2</sub> Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.31 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 8.62 |
| CHEMBL5207885 | — | — | 1 | 8.37 |
| CHEMBL5208751 | — | — | 1 | 8.05 |
| CHEMBL5207405 | — | — | 1 | 8.00 |
| CHEMBL5199628 | — | — | 1 | 7.92 |
| CHEMBL5192961 | — | — | 1 | 7.92 |
| CHEMBL5193621 | — | — | 1 | 7.89 |
| CHEMBL5181318 | — | — | 1 | 7.75 |
| CHEMBL5179440 | — | — | 1 | 7.64 |
| CHEMBL5172250 | — | — | 1 | 7.58 |
| CHEMBL5187046 | — | — | 1 | 7.46 |
| CHEMBL5192496 | — | — | 1 | 7.29 |
| CHEMBL5188374 | — | — | 1 | 7.21 |
| CHEMBL5172734 | — | — | 1 | 7.19 |
| CHEMBL5181341 | — | — | 1 | 7.17 |
| CHEMBL5207214 | — | — | 1 | 7.00 |
| CHEMBL5207597 | — | — | 1 | 6.97 |
| CHEMBL5183482 | — | — | 1 | 6.26 |
| CHEMBL5179419 | — | — | 1 | 6.20 |
| CHEMBL5187312 | — | — | 1 | 6.19 |
| CHEMBL5195053 | — | — | 1 | 6.18 |
| CHEMBL5177490 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL5207885 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL5208751 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5207405 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5199628 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5192961 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5193621 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5181318 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5179440 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5172250 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5187046 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5192496 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL5188374 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL5172734 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL5181341 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL5207214 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL5207597 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL5183482 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL5179419 | — | Ki | = | 638.0 | nM | 6.20 |
| CHEMBL5187312 | — | Ki | = | 646.0 | nM | 6.19 |
| CHEMBL5195053 | — | Ki | = | 654.0 | nM | 6.18 |
| CHEMBL5177490 | — | Ki | = | 1357.0 | nM | 5.87 |