Assay Detail
Binding
CHEMBL5163569
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Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
10
Total Activities
10
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
Long Residence Time at the Vasopressin V<sub>2</sub> Receptor Translates into Superior Inhibitory Effects in <i>Ex Vivo</i> and <i>In Vivo</i> Models of Autosomal Dominant Polycystic Kidney Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.96 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 8.77 |
| CHEMBL5207224 | — | — | 1 | 8.42 |
| CHEMBL5169868 | — | — | 1 | 8.16 |
| CHEMBL5189068 | — | — | 1 | 8.00 |
| CHEMBL5173331 | — | — | 1 | 7.96 |
| CHEMBL5180200 | — | — | 1 | 7.92 |
| CHEMBL5198918 | — | — | 1 | 7.89 |
| CHEMBL5171014 | — | — | 1 | 7.51 |
| CHEMBL5172177 | — | — | 1 | 7.51 |
| CHEMBL5182998 | — | — | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL5207224 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL5169868 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL5189068 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5173331 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5180200 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5198918 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5171014 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5172177 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5182998 | — | Ki | = | 39.0 | nM | 7.41 |