Assay Detail
Binding
CHEMBL817840
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Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Fibroblast |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.34 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.92 |
| CHEMBL165340 | — | — | 1 | 8.89 |
| CHEMBL350869 | — | — | 1 | 8.70 |
| CHEMBL165200 | — | — | 1 | 8.68 |
| CHEMBL349237 | — | — | 1 | 8.59 |
| CHEMBL349141 | — | — | 1 | 8.40 |
| CHEMBL352150 | — | — | 1 | 8.28 |
| CHEMBL351019 | — | — | 1 | 8.15 |
| CHEMBL424163 | — | — | 1 | 8.12 |
| CHEMBL436241 | — | — | 1 | 8.06 |
| CHEMBL164387 | — | — | 1 | 7.94 |
| CHEMBL350408 | — | — | 1 | 7.85 |
| CHEMBL164226 | — | — | 1 | 7.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL165340 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL350869 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL165200 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL349237 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL349141 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL352150 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL351019 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL424163 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL436241 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL164387 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL350408 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL164226 | — | IC50 | = | 14.8 | nM | 7.83 |