Assay Detail
Binding
CHEMBL817919
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Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.55 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307483 | — | — | 1 | 8.92 |
| CHEMBL419667 | RELCOVAPTAN | 2.0 | 1 | 6.75 |
| CHEMBL86577 | — | — | 1 | 6.23 |
| CHEMBL86949 | — | — | 1 | 6.01 |
| CHEMBL89552 | — | — | 1 | 5.75 |
| CHEMBL86667 | — | — | 1 | 5.72 |
| CHEMBL87351 | — | — | 1 | 5.61 |
| CHEMBL87887 | — | — | 1 | 5.61 |
| CHEMBL432375 | — | — | 1 | 5.35 |
| CHEMBL86384 | — | — | 1 | 5.31 |
| CHEMBL86936 | — | — | 1 | 5.18 |
| CHEMBL87455 | — | — | 1 | 5.16 |
| CHEMBL315232 | — | — | 1 | 5.13 |
| CHEMBL315251 | — | — | 1 | 5.09 |
| CHEMBL316093 | — | — | 1 | 5.07 |
| CHEMBL313451 | — | — | 1 | 5.05 |
| CHEMBL315524 | — | — | 1 | 4.99 |
| CHEMBL329209 | — | — | 1 | 4.99 |
| CHEMBL89177 | — | — | 1 | 4.96 |
| CHEMBL314908 | — | — | 1 | 4.84 |
| CHEMBL2112339 | — | — | 1 | 4.84 |
| CHEMBL296908 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307483 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL419667 | RELCOVAPTAN | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL86577 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL86949 | — | Ki | = | 979.0 | nM | 6.01 |
| CHEMBL89552 | — | Ki | = | 1780.0 | nM | 5.75 |
| CHEMBL86667 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL87351 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL87887 | — | Ki | = | 2470.0 | nM | 5.61 |
| CHEMBL432375 | — | Ki | = | 4430.0 | nM | 5.35 |
| CHEMBL86384 | — | Ki | = | 4850.0 | nM | 5.31 |
| CHEMBL86936 | — | Ki | = | 6650.0 | nM | 5.18 |
| CHEMBL87455 | — | Ki | = | 6930.0 | nM | 5.16 |
| CHEMBL315232 | — | Ki | = | 7370.0 | nM | 5.13 |
| CHEMBL315251 | — | Ki | = | 8170.0 | nM | 5.09 |
| CHEMBL316093 | — | Ki | = | 8520.0 | nM | 5.07 |
| CHEMBL313451 | — | Ki | = | 8890.0 | nM | 5.05 |
| CHEMBL315524 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL329209 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL89177 | — | Ki | = | 11100.0 | nM | 4.96 |
| CHEMBL314908 | — | Ki | = | 14300.0 | nM | 4.84 |
| CHEMBL2112339 | — | Ki | = | 14400.0 | nM | 4.84 |
| CHEMBL296908 | — | Ki | > | 10000.0 | nM | - |