Assay Detail
Functional
CHEMBL5163573
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Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| IC50 | 3 | 7.25 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | 4.0 | 1 | 7.95 |
| CHEMBL5173331 | — | — | 1 | 7.03 |
| CHEMBL5198918 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344159 | TOLVAPTAN | IC50 | = | 11.22 | nM | 7.95 |
| CHEMBL5173331 | — | IC50 | = | 93.33 | nM | 7.03 |
| CHEMBL5198918 | — | IC50 | = | 169.82 | nM | 6.77 |