Assay Detail
Binding
CHEMBL820276
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Binding affinity at cloned human Vasopressin V1a receptor stably expressed in CHO cells, using [3H]AVP as radioligand
24
Total Activities
24
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 | 24 | 8.16 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419667 | RELCOVAPTAN | 2.0 | 1 | 9.28 |
| CHEMBL307483 | — | — | 1 | 9.21 |
| CHEMBL86667 | — | — | 1 | 9.00 |
| CHEMBL86949 | — | — | 1 | 8.98 |
| CHEMBL89552 | — | — | 1 | 8.98 |
| CHEMBL2112339 | — | — | 1 | 8.84 |
| CHEMBL432375 | — | — | 1 | 8.67 |
| CHEMBL86577 | — | — | 1 | 8.52 |
| CHEMBL86384 | — | — | 1 | 8.39 |
| CHEMBL87887 | — | — | 1 | 8.35 |
| CHEMBL315232 | — | — | 1 | 8.11 |
| CHEMBL316093 | — | — | 1 | 8.09 |
| CHEMBL86936 | — | — | 1 | 8.04 |
| CHEMBL89177 | — | — | 1 | 8.04 |
| CHEMBL313451 | — | — | 1 | 7.88 |
| CHEMBL87455 | — | — | 1 | 7.86 |
| CHEMBL315524 | — | — | 1 | 7.54 |
| CHEMBL329209 | — | — | 1 | 7.42 |
| CHEMBL314908 | — | — | 1 | 7.41 |
| CHEMBL315251 | — | — | 1 | 7.26 |
| CHEMBL87351 | — | — | 1 | 6.92 |
| CHEMBL330510 | — | — | 1 | 6.67 |
| CHEMBL89015 | — | — | 1 | - |
| CHEMBL296908 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419667 | RELCOVAPTAN | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL307483 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL86667 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL86949 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL89552 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL2112339 | — | Ki | = | 1.46 | nM | 8.84 |
| CHEMBL432375 | — | Ki | = | 2.12 | nM | 8.67 |
| CHEMBL86577 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL86384 | — | Ki | = | 4.09 | nM | 8.39 |
| CHEMBL87887 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL315232 | — | Ki | = | 7.84 | nM | 8.11 |
| CHEMBL316093 | — | Ki | = | 8.09 | nM | 8.09 |
| CHEMBL86936 | — | Ki | = | 9.16 | nM | 8.04 |
| CHEMBL89177 | — | Ki | = | 9.06 | nM | 8.04 |
| CHEMBL313451 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL87455 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL315524 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL329209 | — | Ki | = | 38.3 | nM | 7.42 |
| CHEMBL314908 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL315251 | — | Ki | = | 55.5 | nM | 7.26 |
| CHEMBL87351 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL330510 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL89015 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL296908 | — | Ki | > | 10000.0 | nM | - |